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Sample records for butyrophenones

  1. Receptor-specific positron emission tomography radiopharmaceuticals: 75Br-labeled butyrophenone neuroleptics

    International Nuclear Information System (INIS)

    Cerebral dopaminergic D2 receptors are involved in several common disease states, such as schizophrenia, Parkinson's disease, and Huntington's chorea. The use of radiolabeled D2 receptor-binding ligands with positron emission tomography (PET) to noninvasively quantitate D2 receptor densities thus has potential application in medicine. Butyrophenone neuroleptics have a high in vitro and in vivo binding affinity for cerebral D2 receptors, and due to the useful chemical and nuclear decay properties of 74Br (76% β+, half-life = 1.6 h), the authors have evaluated radiobrominated bromospiperone (BSP), brombenperidol (BBP), and bromperidol (BP) as radiopharmaceuticals for use with PET

  2. Synthesis, Characterization, and Agricultural Biological Activities of 5-Fluoro-2-hydroxy Butyrophenone

    Directory of Open Access Journals (Sweden)

    Fengli Xin

    2013-01-01

    Full Text Available A novel synthetic approach towards 5-fluoro-2-hydroxy butyrophenone is reported. Using 4-fluorophenol as a raw material, the processes of etherification protection, Friedel-Crafts acylation and demethylation provide the target compound under mild conditions. The structure was characterized by the melting point and IR, MS, 1H-NMR, and 13C-NMR spectroscopy. The bioassay results indicate that the target compound exhibits potent antifungal activities against Valsa mali, Coniella dipodiella, and other agricultural plant fungi. The target compound also shows potent herbicidal activities for Lactuca sativa, a dicotyledon, and Echinochloa crus-galli, a monocotyledon. The toxicity regression C50 values of the compound against Valsa mali, Coniothyrium diplodiella, Lactuca sativa seedling, and Echinochloa crusgalli seedling were calculated by SPSS. The Hormesis effect for roots of Echinochloa crusgalli was confirmed.

  3. Synthesis and evaluation of three iodinated haloperidol derivatives as potential dopamine receptor imaging agents

    International Nuclear Information System (INIS)

    Haloperidol, a neuroleptic which shows D-2 receptor affinity and selectivity, has been labelled primarily with positron emitting isotopes. The authors have synthesized three iodinated analogues of Haloperidol to investigate the possibility of an iodine-123 labelled agent for SPECT imaging. These compounds were obtained from the substitution of halogenated butyrophenones by halogenated arylpiperidols. In vitro and in vivo experiments will be discussed

  4. Effects of the Antipsychotic Drug, Haloperidol, on Reproduction in the Fathead Minnow

    Science.gov (United States)

    Haloperidol is a butyrophenone antipsychotic drug used for the treatment of human hyperactive and manic disorders, agitation, and schizophrenia. The drug is thought to act through antagonism of dopaminergic receptors. We have studied a variety of endocrine-disrupting chemicals wi...

  5. Photo- and radiation chemical cycloaddition of maleic acid derivatives to ethylene and acetylene under elavated pressure

    International Nuclear Information System (INIS)

    Based on spectroscopic and kinetic measurements the influence of high pressure on some selected photochemical cycloaddition-reactions is studied. The photo-cycloaddition-reaction of maleic acid anhydride with ethylen has been performed under high ethylen pressures ( 90%). Surprisingly the quantum yield of the cyclo aduct decreases with increasing ethylene pressure from PHI = 0.06 at p = 1 bar to PHI = 0.022 at p = 42 bar. Based on Stern-Volmer quenching experiments, the decrease in ring formation with increasing ethylene concentrations could be explained by an endoergic triplet energy transfer from maleic acid anhydride to ethylene. The type II dissociation of butyrophenone has been quenched also with ethylene. With a lifetime for the first excited butyrophenone triplett state of tau = 6.8 x 10-8 sec, obtained from kinetic data, the velocity constant can be calculated for this reaction with the result k5 = 3 x 106 M-1sec-1. (orig./HK)

  6. Haloperidol Disrupts Opioid-Antinociceptive Tolerance and Physical Dependence

    OpenAIRE

    Yang, Cheng; Chen, Yan; Tang, Lei; Wang, Zaijie Jim

    2011-01-01

    Previous studies from our laboratory and others have implicated a critical role of Ca2+/calmodulin-dependent protein kinase II (CaMKII) in opioid tolerance and dependence. Translational research targeting the CaMKII pathway is challenging, if not impossible, because of a lack of selective inhibitors. We discovered in a preliminary study that haloperidol, a butyrophenone antipsychotic drug, inhibited CaMKII, which led us to hypothesize that haloperidol can attenuate opioid tolerance and depend...

  7. Angioneurotic Edema Associated with Haloperidol

    OpenAIRE

    Samrina Kahlon; Cathy Lee; Roger Chirurgi; Getaw Worku Hassen

    2012-01-01

    Background. Angioneurotic edema is a life-threatening medical emergency that requires urgent diagnosis and treatment. Haloperidol is in the butyrophenone class of antipsychotic medications. Acute anaphylaxis to Haloperidol is very rare and no cases have been reported in literature. Objective. To report the association of life-threatening angioneurotic edema with intramuscular Haloperidol. Case Report. We present a case of an adult with no known allergies in whom angioneurotic edema with tongu...

  8. Drug: D08035 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08035 Drug Haloperidol ... lactate; Haldol (TN) C21H23ClFNO2. C3H6O3 465.1718 465.9422 D08035.gif N ... PSYCHOTICS N05AD Butyrophenone derivatives N05AD01 Haloperidol ... D08035 Haloperidol ... lactate USP drug classification ... [BR:br08302] Antipsychotics 1st Generation/Typical Haloperidol ... D08035 Haloperidol ... lactate Target-based classifica ...

  9. Drug: D00136 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00136 Drug Haloperidol ... (JP16/USP/INN); Haldol (TN) C21H23ClFNO2 375.1401 375.8642 D00136.gif An ... ervous system 117 Psychotropics 1179 Others D00136 Haloperidol ... (JP16/USP/INN) Anatomical Therapeutic Chemical (AT ... PSYCHOTICS N05AD Butyrophenone derivatives N05AD01 Haloperidol ... D00136 Haloperidol ... (JP16/USP/INN) USP drug classif ...

  10. Carrier-added and no-carrier-added syntheses of [18F]spiroperidol and [18F]haloperidol

    International Nuclear Information System (INIS)

    Syntheses of [18F]haloperidol and [18F]spiroperidol in both no-carrier-added and carrier-added forms have been accomplished. The no-carrier-added [18F]butyrophenone neuroleptics were prepared in low (18F-neuroleptics were prepared in better (5-17%) yields by 18F-for-19F nucleophilic aromatic substitution. The preparation of all synthetic precursors, and procedures for radiolabeling are fully described. (author)

  11. Accidental haloperidol poisoning in children

    OpenAIRE

    Gajre, Mona P.; Dimple Jain; Alka Jadhav

    2012-01-01

    Haloperidol, a butyrophenone neuroleptic drug, is an antipsychotic used in the treatment of adult schizophrenia and mania. It is used in children with neurological disorders like chorea and developmental disorders such as hyperactivity. With the advent of newer selective neuroleptics use of haloperidol is now on decline. However, in adults it is still the preferred drug especially in resource challenged settings. Extrapyramidal reactions occur frequently with haloperidol predominantly as park...

  12. Biological reagents and their use

    International Nuclear Information System (INIS)

    The patent relates to a technique for enabling rapid determination of the concentration of neuroleptic drugs such as the phenthiazines and butyrophenones in body fluids of patients. The method is based on the discovery that a neuroleptic drug contained in the body fluid of a patient will successfully compete with the binding of radioactive dopamine receptor site binders to dopamine receptor sites of dopamine receptor material in such a manner that an accurate determination of neuroleptic drug concentration can readily be made. The invention relates to method of radioassay, to a composition of matter for enabling such assays, and to a test kit for the performance of such assays. (U.K.)

  13. Structural determinants of sigma receptor affinity

    International Nuclear Information System (INIS)

    The structural determinants of sigma receptor affinity have been evaluated by examining a wide range of compounds related to opioids, neuroleptics, and phenylpiperidine dopaminergic structures for affinity at sigma receptor-binding sites labeled with (+)-[3H]3-PPP. Among opioid compounds, requirements for sigma receptor affinity differ strikingly from the determinants of affinity for conventional opiate receptors. Sigma sites display reverse stereoselectivity to classical opiate receptors. Multi-ringed opiate-related compounds such as morphine and naloxone have negligible affinity for sigma sites, with the highest sigma receptor affinity apparent for benzomorphans which lack the C ring of opioids. Highest affinity among opioids and other compounds occurs with more lipophilic N-substituents. This feature is particularly striking among the 3-PPP derivatives as well as the opioids. The butyrophenone haloperidol is the most potent drug at sigma receptors we have detected. Among the series of butyrophenones, receptor affinity is primarily associated with the 4-phenylpiperidine moiety. Conformational calculations for various compounds indicate a fairly wide range of tolerance for distances between the aromatic ring and the amine nitrogen, which may account for the potency at sigma receptors of structures of considerable diversity. Among the wide range of structures that bind to sigma receptor-binding sites, the common pharmacophore associated with high receptor affinity is a phenylpiperidine with a lipophilic N-substituent

  14. Structural determinants of sigma receptor affinity

    Energy Technology Data Exchange (ETDEWEB)

    Largent, B.L.; Wikstroem, H.G.; Gundlach, A.L.; Snyder, S.H.

    1987-12-01

    The structural determinants of sigma receptor affinity have been evaluated by examining a wide range of compounds related to opioids, neuroleptics, and phenylpiperidine dopaminergic structures for affinity at sigma receptor-binding sites labeled with (+)-(/sup 3/H)3-PPP. Among opioid compounds, requirements for sigma receptor affinity differ strikingly from the determinants of affinity for conventional opiate receptors. Sigma sites display reverse stereoselectivity to classical opiate receptors. Multi-ringed opiate-related compounds such as morphine and naloxone have negligible affinity for sigma sites, with the highest sigma receptor affinity apparent for benzomorphans which lack the C ring of opioids. Highest affinity among opioids and other compounds occurs with more lipophilic N-substituents. This feature is particularly striking among the 3-PPP derivatives as well as the opioids. The butyrophenone haloperidol is the most potent drug at sigma receptors we have detected. Among the series of butyrophenones, receptor affinity is primarily associated with the 4-phenylpiperidine moiety. Conformational calculations for various compounds indicate a fairly wide range of tolerance for distances between the aromatic ring and the amine nitrogen, which may account for the potency at sigma receptors of structures of considerable diversity. Among the wide range of structures that bind to sigma receptor-binding sites, the common pharmacophore associated with high receptor affinity is a phenylpiperidine with a lipophilic N-substituent.

  15. 3H and 125I radioimmunoassays of haloperidol compared with fluoroimmunoassay involving antibody coupled to magnetizable solid phase

    International Nuclear Information System (INIS)

    Radioimmunoassays for haloperidol are described, involving use of tritium-or 125I-labeled drug or tritium-labeled spiroperidol, and a rabbit antiserum to a drug/bovine serum albumin conjugate. The 125I-labeled drug was prepared by the Chloramine T iodination technique. A fluoroimmunoassay for haloperidol is also described in which the antiserum is coupled to magnetizable solid-phase medium, and fluorescein-labeled haloperidol is used. The assays have acceptable accuracy, precision, and reproducibility, and are specific for haloperidol and similar butyrophenones, with no significant interference from known metabolites and other drugs. Only the radioimmunoassays have sufficient sensitivity to cover the whole range of haloperidol concentrations in serum. The fluoroimmunoassay can be used to monitor high concentrations of haloperidol in 150 μL samples or the complete concentration range of 1-mL serum samples that are extracted and concentrated before assay

  16. 3H and 125I radioimmunoassays of haloperidol compared with fluoroimmunoassay involving antibody coupled to magnetizable solid phase

    International Nuclear Information System (INIS)

    Radioimmunoassays for haloperidol are described, involving use of tritium- or 125I-labeled drug or tritium-labeled spiroperidol, and a rabbit antiserum to a drug/bovine serum albumin conjugate. The 125I-labeled drug was prepared by the Chloramine T iodination technique. A fluoroimmunoassay for haloperidol is also described in which the antiserum is coupled to magnetizable solid-phase medium, and fluorescein-labeled haloperidol is used. The assays have acceptable accuracy, precision, and reproducibility, and are specific for haloperidol and similar butyrophenones, with no significant interference from known metabolites and other drugs. Only the radioimmunoassays have sufficient sensitivity to cover the whole range of haloperidol concentrations in serum. The fluoroimmunoassay can be used to monitor high concentrations of haloperidol in 150-microL samples or the complete concentration range of 1-mL serum samples that are extracted and concentrated before assay

  17. On the clinical impact of cerebral dopamine D2 receptor scintigraphy

    International Nuclear Information System (INIS)

    The present review describes findings and clinical indications for the dopamine D2 receptor scintigraphy. Methods for the examination of D2 receptors are positron emission tomography (PET) using 11C- or 18F-labelled butyrophenones or benzamides or single photon emission tomography (SPECT) using 123I-iodobenzamide (IBZM) respectively. The most important indication in neurology is the differential diagnosis of Parkinsonism: Patients with early Parkinson's disease show an increased D2 receptor binding (D2-RB) compared to control subjects. However, patients suffering from Steele-Richardson-Olszewski-Syndrome or Multiple System Atrophy show a decreased D2-RB and are generally non-responsive to treatment. Postsynaptic blockade of D2 receptors results in a drug induced Parkinsonian syndrome, which can be diagnosed by D2 scintigraphy. Further possible indications occur in psychiatry: The assessment of receptor occupancy is useful in schizophrenic patients treated with neuroleptics. Additionally, D2 receptor scintigraphy might help to clarify the differential diagnosis between neuroleptic malignant syndrome and lethal catatonia. The method might be useful for supervising neurobiochemical changes in drug dependency and during withdrawal. Assessment of dopamine D2 receptor binding can simplify the choice of therapy in depressive disorder: Patients showing a low D2 binding are likely to improve following an antidepressive drug treatment whereas sleep deprivation is promising in patients with high D2 binding. (orig.)

  18. Imaging dopamine transmission in schizophrenia

    International Nuclear Information System (INIS)

    Over the last ten years, several positron emission tomography (PET) and single photon computerized tomography (SPECT) studies of the dopamine (DA) system in patients with schizophrenia were performed to test the hypothesis that DA hyperactivity is associated with this illness. In this paper are reviewed the results of fifteen brain imaging studies comparing indices of DA function in drug naive or drug free patients with schizophrenia and healthy controls: thirteen studies included measurements of Da D2 receptor density, two studies compared amphetamine-induced DA release, and two studies measured DOPA decarboxylase activity, an enzyme involved in DA synthesis. It was conducted a meta-analysis of the studies measuring D2 receptor density parameters, under the assumption that all tracers labeled the same population of D2 receptors. This analysis revealed that, compared to healthy controls, patients with schizophrenia present a significant but mild elevation of D2 receptor density parameters and a significant larger variability of these indices. It was found no statistical evidence that studies performed with radiolabeled butyrophenones detected a larger increase in D2 receptor density parameters than studies performed with other radioligands, such as benzamides. Studies of presynaptic activity revealed an increase in DA transmission response to amphetamine challenge, and an increase in DOPA decarboxylase activity. Together, these data are compatible with both pre- and post-synaptic alterations of DA transmission in schizophrenia. Future studies should aim at a better characterization of these alterations, and at defining their role in the pathophysiology of the illness

  19. Formulation and evaluation of melt-in-mouth tablets of haloperidol

    Directory of Open Access Journals (Sweden)

    Jha Sajal

    2008-01-01

    Full Text Available Haloperidol, a butyrophenone, is widely used neuroleptic. Though haloperidol is well absorbed after oral dosing, there is a first pass metabolism leading to a reduced bioavailability of the drug (60-70%. Therefore, the present investigation is concerned with the development of melt-in-mouth tablets of haloperidol. Various formulations were prepared incorporating a combination of superdisintegrants, croscarmellose sodium, sodium starch glycolate, and crospovidone by direct compression method. The formulated melt-in-mouth tablets were evaluated for various physicochemical parameters, disintegration time and for in vitro drug release. All the formulations had disintegration time less than 30 s and release maximum amount of drug by 12 min. Formulation containing higher concentration of crospovidone decreases disintegration time and optimize the drug release. The most satisfactory formulation was found to be stable during the stability studies conducted as per ICH guidelines QIC, as it showed no significant changes ( P < 0.05 in the physicochemical properties, disintegration time and in vitro drug release.

  20. Alteration of dopamine receptor sensitivity by opiates and the subsequent effect of this alteration on opiate tolerance and dependence

    Energy Technology Data Exchange (ETDEWEB)

    Martin, J.R.

    1985-01-01

    The present study was undertaken to determine whether there is an alteration of dopamine receptor sensitivity following opiate administration, and whether this alteration has any influence on the development of opiate tolerance and dependence. Behavioral hypersensitivity to direct-acting dopamine agonists was observed in mice following acute or chronic morphine administration. Acute levorphanol administration also resulted in potentiation of dopamine agonist-induced behaviors. An increase in density of dopamine receptors, as measured by (/sup 3/H)butyrophenone binding accompanied the development of behavioral hypersensitivity. This increase was localized to the striatum, an area important in the mediation of dopamine-agonist induced behaviors. Naloxone or LiCl coadministered with the opiates prevented the development of hypersensitivity and the increase in density of dopamine receptors. Coadministration of lithium enhanced the development of acute and chronic tolerance. Lithium enhanced the development of dependence as determined by naloxone-induced hypothermia in chronically morphine-treated mice. Apomorphine enhanced naloxone-induced withdrawal in acutely dependent mice. This enhancement was blocked by coadministration of lithium with the opiates. These results suggest that dopamine receptor supersensitivity influences the degree of tolerance and dependence.

  1. Method validation and measurement uncertainty for the simultaneous determination of synthetic phenolic antioxidants in edible oils commonly consumed in Korea.

    Science.gov (United States)

    Kim, Jae-Min; Choi, Seung-Hyun; Shin, Gi-Hae; Lee, Jin-Ha; Kang, Seong-Ran; Lee, Kyun-Young; Lim, Ho-Soo; Kang, Tae Seok; Lee, Ok-Hwan

    2016-12-15

    This study investigated a method for the validation and determination of measurement uncertainty for the simultaneous determination of synthetic phenolic antioxidants (SPAs) such as propyl gallate (PG), octyl gallate (OG), dodecyl gallate (DG), 2,4,5-trihydroxy butyrophenone (THBP), tert-butylhydroquinone (TBHQ), butylated hydroxyanisole (BHA), and butylated hydroxytoluene (BHT) in edible oils commonly consumed in Korea. The validated method was able to extract SPA residues under the optimized HPLC-UV and LC-MS/MS conditions. Furthermore, the measurement of uncertainty was evaluated based on the precision study. For HPLC-UV analysis, the recoveries of SPAs ranged from 91.4% to 115.9% with relative standard deviations between 0.3% and 11.4%. In addition, the expanded uncertainties of the SPAs ranged from 0.15 to 5.91. These results indicate that the validated method is appropriate for the extraction and determination of SPAs and can be used to verify the safety of edible oil products containing SPAs residues. PMID:27451150

  2. Evaluation of intravenous lipid emulsion on haloperidol-induced hypotension in rabbits.

    Science.gov (United States)

    Moshiri, Mohammad; Vahabzadeh, Maryam; Mohammadpour, Amir Hooshang; Hosseinzadeh, Hossein

    2016-05-01

    There are many reports on the effects of intravenous lipid emulsion (ILE) as an antidote in drug toxicity. Haloperidol (HAL) is a butyrophenone antipsychotic agent which is highly lipophilic. Hypotension is an important adverse effect of HAL administration and overdose. The aim of this study was to investigate the beneficial hemodynamic effects of ILE on acute HAL poisoning. We used six groups of five male rabbits. Two groups received aseptic distilled water intravenously followed by infusion of 18.6 ml/kg normal saline, as negative control group, or ILE 20% after 0.5 h. The third group received 18.6 ml/kg normal saline after HAL infusion (2.6 mg/kg). The other three groups received ILE 20% solution (6, 12, and 18.6 ml/kg) following HAL (2.6 mg/kg) administration. We measured blood pressure at 0, 0.5, 1, 2, 3, 4, 8, and 24 h after starting HAL administration, from left forelimb using a noninvasive method that was carried out automatically with a neonatal intensive care unit bedside monitor. ILE 20% at the dose of 18 ml/kg could return the reduced mean arterial pressure and diastolic blood pressure sooner than the other doses and normal saline. In conclusion, ILE could reverse HAL-induced hypotension same as the other lipophilic drugs. However, the clinical use of ILE for this purpose needs more evaluation to determine its exact indication and safety. PMID:24444695

  3. [3H]Spiroxatrine labels a serotonin/sub 1A/-like site in the rat hippocampus

    International Nuclear Information System (INIS)

    [3H]Spiroxatrine was examined as a potential ligand for the labeling of 5-HT/sub 1A/ sites in the rat hippocampus. Analysis o the binding of [3H]spiroxatrine in the absence and presence of varying concentrations of three monoamine neurotransmitters revealed that serotonin (5-HT) had high affinity for the [3H]spiroxatrine binding sites, consistent with the labeling of 5-HT1 sites, while dopamine and norepinephrine had very low affinity. Saturation studies of the binding of [3H]spiroxatrine revealed a single population of sites with a K/sub d/ = 2.21 nM. Further pharmacologic characterization with the 5-HT/sub 1A/ ligands 8-hydroxy-2-(di-ni-propylamino)tetralin, ipsapirone, and WB4101 and the butyrophenone compounds spiperone and haloperidol gave results that were consistent with [3H]spiroxatrine labeling 5-HT/sub 1A/ sites. This ligand produced stable, reproducible binding with a good ratio of specific to nonspecific binding. The binding of [3H]spiroxatrine was sensitive to GTP, suggesting that this ligand may act as an agonist. 21 references, 5 figures, 2 tables

  4. [Treatment of blepharospasm with botulinum toxin].

    Science.gov (United States)

    Pikielny, R T; Micheli, F E; Fernández Pardal, M M; Casas Parera, I; Giannaula, R J; Gatto, M

    1990-01-01

    Blepharospasm is a relatively frequent cranial dystonia which may be seen either alone or related to orofacial-mandibular dystonia (Meige's syndrome). In its maximum degree it can cause functional blindness.Twelve patients with blepharospasm (4 essential and 8 Meige's syndrome) who had been previously treated unsuccessfully with drugs (trihexyphenidyl, biperiden, carbamazepine, lithium, baclofen, lisuride, imipramine, clonazepam and butyrophenones) were treated for 12 months with periocular injections of botulinum toxin (BOTOX). A "low" dose of 12,5 U per eye was employed. With this dose, eleven out of twelve patients experienced significant improvement which lasted from five to fifteen weeks. The only nonresponder obtained complete relief upon duplicating the dose. The only side effect was uni or bilateral ptosis in six patients which improved completely in seven to twenty one days. One patient developed a peripheral facial palsy with complete remission in nineteen days. No systemic side effects were noted. There was only one desertion from this study due to depression enhanced by prolonged (21 days) ptosis. All patients (including the deserter) agreed that treatment with BOTOX provided more relief than any other previous therapeutic method. Our results confirm those obtained by others but a more prolonged study is needed to better evaluate long term effects. PMID:2101846

  5. Alteration of dopamine receptor sensitivity by opiates and the subsequent effect of this alteration on opiate tolerance and dependence

    International Nuclear Information System (INIS)

    The present study was undertaken to determine whether there is an alteration of dopamine receptor sensitivity following opiate administration, and whether this alteration has any influence on the development of opiate tolerance and dependence. Behavioral hypersensitivity to direct-acting dopamine agonists was observed in mice following acute or chronic morphine administration. Acute levorphanol administration also resulted in potentiation of dopamine agonist-induced behaviors. An increase in density of dopamine receptors, as measured by [3H]butyrophenone binding accompanied the development of behavioral hypersensitivity. This increase was localized to the striatum, an area important in the mediation of dopamine-agonist induced behaviors. Naloxone or LiCl coadministered with the opiates prevented the development of hypersensitivity and the increase in density of dopamine receptors. Coadministration of lithium enhanced the development of acute and chronic tolerance. Lithium enhanced the development of dependence as determined by naloxone-induced hypothermia in chronically morphine-treated mice. Apomorphine enhanced naloxone-induced withdrawal in acutely dependent mice. This enhancement was blocked by coadministration of lithium with the opiates. These results suggest that dopamine receptor supersensitivity influences the degree of tolerance and dependence

  6. Imaging dopamine transmission in schizophrenia

    Energy Technology Data Exchange (ETDEWEB)

    Laruelle, M. [New York, Columbia Univ. College of Physicians and Surgeons, NY (United States). New York State Psychiatric Insitute. Brain Imaging Division

    1998-09-01

    Over the last ten years, several positron emission tomography (PET) and single photon computerized tomography (SPECT) studies of the dopamine (DA) system in patients with schizophrenia were performed to test the hypothesis that DA hyperactivity is associated with this illness. In this paper are reviewed the results of fifteen brain imaging studies comparing indices of DA function in drug naive or drug free patients with schizophrenia and healthy controls: thirteen studies included measurements of Da D{sub 2} receptor density, two studies compared amphetamine-induced DA release, and two studies measured DOPA decarboxylase activity, an enzyme involved in DA synthesis. It was conducted a meta-analysis of the studies measuring D{sub 2} receptor density parameters, under the assumption that all tracers labeled the same population of D{sub 2} receptors. This analysis revealed that, compared to healthy controls, patients with schizophrenia present a significant but mild elevation of D{sub 2} receptor density parameters and a significant larger variability of these indices. It was found no statistical evidence that studies performed with radiolabeled butyrophenones detected a larger increase in D{sub 2} receptor density parameters than studies performed with other radioligands, such as benzamides. Studies of presynaptic activity revealed an increase in DA transmission response to amphetamine challenge, and an increase in DOPA decarboxylase activity. Together, these data are compatible with both pre- and post-synaptic alterations of DA transmission in schizophrenia. Future studies should aim at a better characterization of these alterations, and at defining their role in the pathophysiology of the illness.

  7. Mild and effective aliphatic and aromatic n.c.a. /sup 18/F-fluorination using crown ether

    International Nuclear Information System (INIS)

    For nucleophilic substitution with [/sup 18/F]-fluoride in crown ether-catalyzed reactions, the aminopolyether 2.2.2. (Kryptofix, Merck)-K/sub 2/CO/sub 3/ complex in acetonitrile was found to be optimal. The method was further optimized and applied to n.c.a. /sup 18/F-labeling. /sup 18/F-fluoroacetate and /sup 18/F-heptadecanoic acid were prepared with 92 +- 3% radiochemical yield and a specific activity of > 15000 Ci/nmole. Compared to other methods, the reaction in the presence of the crown ether is less sensitive and allows simpler routine production. The mild conditions of the new reaction system also allows the production of the fluoromethylation agent /sup 18/FCH/sub 2/Br. Starting from CH/sub 2/Br/sub 2/ the use of CH/sub 2//sup 18/F instead of /sup 11/CH/sub 3/ makes available longer lived /sup 18/F-analogue tracers. The feasibility was demonstrated by n.c.a. fluoromethylation of phenolate and piperidine with radiochemical yields of 15 to 20%. The highest potency of the crown ether-supported reaction lies in the significantly increased efficiency of nucleophilic aromatic fluorination. Thus replacement of a nitro group in dinitrobenzene was accomplished within two minutes in acetonitrile-crown ether-K/sub 2/CO/sub 3/ even at 800C with 80 +- 3%. In comparison in DMSO without crown ether and in acetamide melt yields of 80 +- 2% and 40 +- 4%, respectively, were only obtained at 1500C. In DMSO-crown ether the labeling of p-nitro-benzonitril is almost independent of the reaction temperature from 600C to 1800C. Thus temperature-sensitive molecules such as butyrophenones can be efficiently fluorinated under mild conditions

  8. Development of [11C]-α-aminoisobutyric acid and [18F]-haloperidol as substrate-specific radiotracers

    International Nuclear Information System (INIS)

    In light of the emergence of positron emission tomography (PET), two new substrate-specific radiotracers have been synthesized and evaluated as potential agents for the study of specific physiological processes: [1-11C]-α-aminoisobutyric acid ([1-11C]-AIB), a transport system-specific radiotracer for tumor localization and for the assessment of amino acid transport in vivo; and [18F]-haloperidoll, a receptor-binding radiotracer for the assessment of brain dopamine receptors in vivo. AIB, a non-metabolized amino acid, accumulates in cells, particularly malignant cells, via the A type, or ''alanine-preferring'', amino acid transport system [1-11C]-AIB in normal and in treated and untreated tumor-bearing rats, in tumor-bearing dogs, and in a tumor-bearing patient indicate rapid blood clearance and, concomitantly, rapid tissue localization, with slow net redistribution. Generally, there was selective localization in the kidney, in the liver, and in the pancreas, as well as in various tumors. The canine tumors and the human tumor were well visualized by external scintigraphy, especially when utilizing PET. [18F]-Haloperidol, a dopamine receptor-binding neuroleptic of the butyrophenone series widely used in the management of schizophrenia was prepared via the Balz-Schiemann reaction. As the haloperdol dose administered to mice was increased from 0.01 to 1000 μg/kg, the relative concentration (μCi found per gm tisue sample/μCi injected per gm body mass) of [18F]-haloperidol at 1 hr decreased from 30 to 1.0 in the striatum and from 8.0 to 1.0 in the cerebellum. The decrease in striatum radioactivity reflects competition between labeled and unlabeled haloperidol for dopamine receptors

  9. Perbandingan Granisetron 0,01 mg/KgBb dengan Ondansetron 0,08 Mg/Kg.Bb Untuk Mencegah Mual Muntah Pascaoperasi Dini Mastektomi Radikal Modifikasi

    Directory of Open Access Journals (Sweden)

    Budi Fitriyana

    2013-04-01

    Full Text Available Postoperative nausea and vomiting not only cause discomfort to the patient, but also lead to electrolyte imbalance, regurgitation and aspiration, bleeding and loss of surgical sutures. Patients who experience postoperative nausea and vomiting will require further attention and treatment which of course increases the cost of medical services. Women who underwent mastectomy with accompanying decision underarm lymph nodes have a high risk of postoperative nausea and vomiting. Many anti-vomiting are given including antihistamines, butyrophenon, and dopamine receptor antagonists have been reported to have undesirable side effects including excessive sedation, hypotension, dry mouth, dysphoria, hallucinations and extrapyramidal effects. 5 HT3 receptor antagonists provide a major advancement for treatment of postoperative nausea and vomiting due to fewer side effects when compared with anti-vomiting medications before. This study will compare the two drugs 5 HT3 receptor antagonist granisetron with ondansetron in preventing postoperative nausea and vomiting modified radical mastectomy early. Conducted research on 58 patients ASA I and II modified radical mastectomy is performed under general anesthesia. Sampling was carried out using double-blind randomized controlled trial. Samples were divided into two groups by block randomization. Group G is given granisetron 0.01 gr / kg.bb and group O is given ondansetron 0.08 mg / kg.bb. Drug treatment is administered intravenously 30 minutes before the surgery ended on a complete evaluation of blood pressure, heart rate, oxygen saturation and length of surgery. Postoperative nausea and vomiting shortly after surgery assessed every hour until 6 hours after surgery (early postoperative nausea and vomiting to 4 scale (0-3. Data were analyzed by t-test, Chi-square test, Mann-Whitney test and Fisher's Exact test on Windows SPSS ver.16 The results suggest there is a tendency complaints of postoperative nausea and

  10. On the clinical impact of cerebral dopamine D{sub 2} receptor scintigraphy; Zur klinischen Wertigkeit der zerebralen Dopamin-D{sub 2}-Rezeptorszintigraphie

    Energy Technology Data Exchange (ETDEWEB)

    Larisch, R. [Duesseldorf Univ. (Germany). Klinik fuer Nuklearmedizin; Klimke, A. [Duesseldorf Univ. (Germany). Psychiatrische Klinik

    1998-12-31

    The present review describes findings and clinical indications for the dopamine D{sub 2} receptor scintigraphy. Methods for the examination of D{sub 2} receptors are positron emission tomography (PET) using {sup 11}C- or {sup 18}F-labelled butyrophenones or benzamides or single photon emission tomography (SPECT) using {sup 123}I-iodobenzamide (IBZM) respectively. The most important indication in neurology is the differential diagnosis of Parkinsonism: Patients with early Parkinson`s disease show an increased D{sub 2} receptor binding (D{sub 2}-RB) compared to control subjects. However, patients suffering from Steele-Richardson-Olszewski-Syndrome or Multiple System Atrophy show a decreased D{sub 2}-RB and are generally non-responsive to treatment. Postsynaptic blockade of D{sub 2} receptors results in a drug induced Parkinsonian syndrome, which can be diagnosed by D{sub 2} scintigraphy. Further possible indications occur in psychiatry: The assessment of receptor occupancy is useful in schizophrenic patients treated with neuroleptics. Additionally, D{sub 2} receptor scintigraphy might help to clarify the differential diagnosis between neuroleptic malignant syndrome and lethal catatonia. The method might be useful for supervising neurobiochemical changes in drug dependency and during withdrawal. Assessment of dopamine D{sub 2} receptor binding can simplify the choice of therapy in depressive disorder: Patients showing a low D{sub 2} binding are likely to improve following an antidepressive drug treatment whereas sleep deprivation is promising in patients with high D{sub 2} binding. (orig.) [Deutsch] Die vorliegende Arbeit gibt eine Uebersicht ueber Befunde und klinische Indikationen zur Dopamin-D{sub 2}-Rezeptorszintigraphie. Methoden zur Untersuchung der D{sub 2}-Rezeptoren sind die Positronen-Emissions-Tomographie (PET) mit {sup 11}C- oder {sup 18}F-markierten Butyrophenonen oder Benzamiden oder die Einzelphotonen-Emissions-Tomographie (SPECT) mit {sup 123}I

  11. Azaperone e sua associação com xilazina ou dexmedetomidina em suínos Azaperone and its association with xilazina or dexmedetomidina in swines

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    Fabíola Niederauer Flôres

    2009-07-01

    Full Text Available O estudo objetivou avaliar o efeito sedativo do azaperone e de sua associação com a xilazina ou dexmedetomidina na espécie suína, assim como verificar a possibilidade de o agente butirofenônico contrabalançar os efeitos causados pelos agonistas α2-adrenérgicos nos parâmetros cardiovasculares. Foram estudados 18 suínos hígidos da linhagem Dambread X MS 50, de 50 dias de idade, pesando 17,3kg (±1,7. Todos os animais foram submetidos a anestesia com isofluorano para instrumentação necessária ao protocolo experimental e, 30 minutos após a recuperação anestésicas, os parâmetros basais foram mensurados e os animais alocados aleatoriamente em três grupos de seis animais cada: GA (Azaperone 2mg kg-1 + Cloreto de sódio 0,5ml - IM, GAD (Azaperone 2mg kg-1 + Dexmedetomidina 3µg kg-1 - IM, GAX (Azaperone 2mg kg-1 + Xilazina 2mg kg-1 - IM. Os parâmetros foram novamente avaliados aos 15, 30, 45 e 60 minutos após administração dos fármacos correspondentes aos grupos do estudo. A frequência cardíaca teve seus valores reduzidos em todos os grupos, porém essa redução foi maior no GAX. Durante o estudo não foi observado efeito bifásico sobre a pressão arterial, com hipertensão seguida de hipotensão. O GAX apresentou redução de PaO2 e aumento de PaCO2, assim como observou-se melhor efeito sedativo nesse grupo. Os resultados permitem concluir que a associação de azaperone com xilazina promoveu melhor sedação e miorrelaxamento e menor resposta a estímulos.The aim of this study was to evaluate the sedative effects of azaperone and its association with xylazine or dexmedetomidine in swine, as well as verifying the possibility of the butyrophenone agent to counterbalance the effects caused by α2-adreneceptor agonists on the cardiovascular and hemodynamic parameters. For this, eighteen healthy swines of the Dambread X MS 50 lineage aged 50 days-old, weighing around 17.3kg (±1.7 were used. All animals were submitted an

  12. Study on the variation rules of material basis of Rhubarb after processing%大黄饮片炮制前后物质基础变化规律研究

    Institute of Scientific and Technical Information of China (English)

    李丽; 肖永庆

    2012-01-01

    Objective: To reveal the variation rules of Rhubarb after processing, according to comparison of chemical constituents and biological activities in three commonly used pieces from Rhubarb. Methods: we conducted a systematic chemical study on Rheum palmatum L. By organic solvent extraction and chromatographic separation. The HPLC fingerprint and the content of main constituents were used to qualitative and quantitative evaluation respectively. At the same time, a new simulation processing method were used to verify the variation of Rhubarb before and after processing which was taking the blank pieces as the carrier and filled in different chemical constituents. Results: There were thirty-four compounds identified from Rheum palmatum L. Including four new compounds. The HPLC fingerprint in two detection wavelengths and the contents of 17 main chemical components among five pieces indicated that the changes were significantly in the braising with liquor and the charring pieces compare with the crude pieces. The content of anthraquinone glycosides were reduced by 55% and 95%, while the total anthraquinone aglycones increased by 75% and 46% in the braising with liquor and the charring pieces. In addition, the content of gallic acid was sharply increased about 2.4 times in the braising pieces. Diarrhea and antipyretic pharmacological experiments showed that the crude pieces have the strongest purgative and febrifuge effect; on the contrary, the braised and the charred pieces had no diarrhea effect. Conclusion: The "bitter and cold" property of Rhubarb is gradually decreased from crude pieces, braising with liquor to charring pieces by the chemical and biological analysis. Meanwhile, the diarrhea intensity which based on the modern pharmacodynamic study is gradually reduced by the same order. The change rules are closely related to the decrease in compound tanning, anthraquinone glucoside, butyrophenone glucoside and the increase in gallic acid, anthraquinone compounds

  13. 住院精神障碍患者跌倒致伤的情况分析%Analysis on Injury Cases of Fall Down of Mental Disorder Inpatients

    Institute of Scientific and Technical Information of China (English)

    傅慕君; 诸惠萍; 周莉莉; 吴微

    2012-01-01

    Objective To provide basis for the effective management of fall down hy analyzing the injury cases of fall down of mental disorder inpatients.Methods The data of 85 cases of mental disorder inpatients who developed fall down from 2006 to 2010 were analyzed retrospectively on their age,psychotropic medication,combined diseases and type of injury.Results Of 85 mental disorder inpatients who developed fall down,38 were observed with history oi chronic diseases including 15 cased of hypertension(39, 5%),10 cases of diabetes(26.3%) and 5 cases of heart diseases(13.2%).Fracture was the main injury types of fall down of mental disorder inpatients.The incidence of forearm fracture of upper limb was the highest.The highest incidence of fracture (55.9%) was observed in patients aged 50 — 70 years.For those below 50 years old, the incidences of open injury,head injury and soft tissue injury were 22.6/1),12.9% and 25.8% respectively.For the psychiatric patients treated v/ith classic drug treatment (traditional anti-mental disorder drugs, including the phenothiazines, Thioxanthone,butyrophenone,benzene lactam drugs),the incidences of fractures,open injuries,brain damage and soft tissue injury were 36.4% ,26.9%, 13.6% and 21.1%, respectively.Conclusion Fall down is quite common among mental disorder inpatients, so we should improve the cognition of fall risk, take effective preventive measures and reduce healthy injury of fall down.%目的 了解住院精神障碍患者跌倒致伤情况,为预防跌倒的科学管理提供依据.方法 回顾性分析2006-2010年在上海市民政第二精神卫生中心住院期间发生跌倒致伤的85例患者的年龄、精神科用药、合并疾病以及损伤类型等情况.结果 85例发生跌倒的精神障碍患者中,38例有合并慢性病史,其中高血压者15例,占39.5%;糖尿病者10例,占26.3%;心脏疾病者5例,占13.2%.精神障碍患者跌倒后的损伤主要为骨折,以前臂及手指骨骨折最多见.50~70