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Sample records for butyrophenones

  1. Optimization studies concerning the direct nucleophilic fluorination of butyrophenone neuroleptics

    Energy Technology Data Exchange (ETDEWEB)

    Katsifis, A; Hamacher, K; Schnitter, J; Stoecklin, G [Forschungszentrum Juelich GmbH (Germany). Inst. fuer Chemie 1 - Nuklearchemie

    1993-07-01

    Based on the direct nucleophilic aromatic substitution described previously for [[sup 18]F]N-methylspiperone the butyrophenone neuroleptics benperidol, droperidol, fluanisone and haloperidol were labelled with fluorine-18. The n.c.a. aromatic nucleophilic NO[sub 2] [yields] [sup 18]F substitution takes place in the presence of the moderately basic cryptate system consisting of Kryptofix 2.2.2., potassium oxalate and potassium carbonate. The one step labeling reaction was performed in different solvents and is equally successful in dimethylsulfoxide, dimethylformamide or dimethylacetamide yielding 25-35% (EOS) within a reaction time of 5-30 min in the range of 140-160[sup o]C at analytical activity levels. (author).

  2. The rapid synthesis of high purity [{sup 18}F]butyrophenone neuroleptics from nitro precursors for PET study

    Energy Technology Data Exchange (ETDEWEB)

    Hashizume, Kazunari; Hashimoto, Naoto; Kato, Hiroo; Cork, D G; Miyake, Yoshihiro [National Cardiovascular Center, Suita, Osaka (Japan)

    1995-04-01

    We have completed rapid syntheses of [{sup 18}F]butyrophenone neuroleptics ([{sup 18}F]haloperidol and [{sup 18}F]spiperone) from their nitro precursors in high radiochemical yields (up to 21%) by combining a one-step nitro-fluoro exchange reaction and a novel high performance liquid chromatography (HPLC) separation method. The synthesis time was ca. 95 min and both the radiochemical and chemical purities of the labeled products were over 99%. (author).

  3. Comparison of three /sup 18/F-labeled butyrophenone neuroleptic drugs in the baboon using positron emission tomography

    Energy Technology Data Exchange (ETDEWEB)

    Arnett, C D; Shiue, C Y; Wolf, A P; Fowler, J S; Logan, J; Watanabe, M

    1985-03-01

    The butyrophenone neuroleptics spiroperidol, benperidol, and haloperidol were radiolabeled with fluorine-/sup 18/ and studied in baboon brain using positron emission transaxial tomography (PETT). Pretreatment of the baboon with a high pharmacological dose of (+)-butaclamol reduced the specifically bound component of radioactivity distribution in the striatum to approximately the radioactivity distribution found in the cerebellum. Comparative studies of brain distribution kinetics over a 4-h period indicated that either (/sup 18/F)spiroperidol or (/sup 18/F)benperidol may be suitable for specific labeling of neuroleptic receptors. In an 8-h study with (/sup 18/F)spiroperidol, striatal radioactivity did not decline, suggesting that spiroperidol either has a very slow dissociation rate or that it binds irreversibly to these receptors in vivo. (/sup 18/F)Haloperidol may not be suitable for in vivo PETT studies, because of a relatively high component of nonspecific distribution and a faster dissociation from the receptor. Analysis of /sup 18/F in plasma after injection of (/sup 18/F)spiroperidol indicated rapid metabolism to polar and acidic metabolites, with only 40% of the total radioactivity being present as unchanged drug after 30 min. Analysis of the metabolic stability of the radioactively labeled compound in rat striatum indicated that greater than 95% of (/sup 18/F)spiroperidol remains unchanged after 4 h.

  4. Radiosynthesis and pharmacokinetics of high specific activity /sup 75,77/Br-bromperidol, a potent butyrophenone neuroleptic

    International Nuclear Information System (INIS)

    Moerlein, S.M.; Stocklin, G.

    1984-01-01

    Bromperidol, 4-[4-(4-bromophenyl)-4-hydroxypiperidino]-4'- fluorobutyrophenone, is a potent neuroleptic which has found clinical use in the treatment of schizophrenia. Of the major dopaminergic receptor-binding ligands, bromperidol has the greatest specificity for binding to cerebral dopamine receptors (K/sub i/ = 3.7 nM) relative to competitive cerebral serotonin (K/sub i/ = 26 nM), α-adrenergic (K/sub i/ = 100 nM) or histamine (K/sub i/ = 700 nM) receptors. The authors have therefore prepared bromperidol labelled with no-carrier-added (n.c.a.) /sup 75/Br (t/sub 1/2/ = 1.6 hr β/sup +/) or /sup 77/Br (t/sub 1/2/ = 52 hr EC) for evaluation as a radiopharmaceutical for mapping cerebral dopamine receptor areas with PECT technology, as well as for non-invasive pharmacodynamic studies in man with conventional nuclear medicine equipment. 4-[4-(4-trimethylstannylphenyl)-4-hydroxypiperidino]-4'- fluorobutyrophenone, TMSn-P, was synthesized in 40% chemical yield by reaction of trimethylstannyl sodium with bromperidol. TMSn-P was purified by preparative HPLC and characterized by /sup 1/H-NMR and GC-MS. TMSn-P was radiobrominated in methanol using n.c.a. /sup 75/Br/sup -/ or /sup 77/Br/sup -/ and dichloramine-T as oxidizing agent. Product /sup 75,77/Br-bromperidol was separated from impurities, including chlorinated side-product halo-peridol, using HPLC (RP-18; MeOH/H/sub 2/O/Et/sub 3/N = 70/30/0.3). For a reaction time of 5 minutes, and an overall radiopharmaceutical production time of 30 minutes, /sup 75,77/Br-bromperidol was obtained in physiological saline solution with 40% radiochemical yield and a specific activity > 10,000 Ci/mmole. The pharmacokinetics in rodents and PECT studies in primates using /sup 75,77/Br-bromperidol are compared with that of previously-reported /sup 75,77/Br-brombenperidol

  5. Dgroup: DG00887 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG00887 Chemical ... DGroup Melperone ... D07309 ... Melperone (INN) D08172 ... Melperone hydrochloride Neuropsychiatr...ic agent ... DG01940 ... Butyrophenone derivative ATC code: N05AD03 Butyrophenone antipsychotics ...

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

    International Nuclear Information System (INIS)

    Hunter, D.H.; Strickland, L.A.; Zabel, P.L.

    1990-01-01

    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

  7. 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...

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

    International Nuclear Information System (INIS)

    Mirbach, M.

    1975-01-01

    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 k 5 = 3 x 10 6 M -1 sec -1 . (orig./HK) [de

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

    International Nuclear Information System (INIS)

    Kilbourn, M.R.; Welch, M.J.; Dence, C.S.; Tewson, T.J.; Saji, H.; Maeda, M.

    1984-01-01

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

  10. Carrier-added and no-carrier-added syntheses of (/sup 18/F)spiroperidol and (/sub 18/F)haloperidol

    Energy Technology Data Exchange (ETDEWEB)

    Kilbourn, M R; Welch, M J; Dence, C S; Tewson, T J; Saji, H; Maeda, M

    1984-07-01

    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 (less than 2%) yield by acid decomposition of aryl piperidine triazenes. Carrier-added 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.

  11. Biological reagents and their use

    International Nuclear Information System (INIS)

    1981-01-01

    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.)

  12. Carrier-added and no-carrier-added syntheses of (/sup 18/F)spiroperidol and (/sup 18/F)haloperidol

    Energy Technology Data Exchange (ETDEWEB)

    Kilbourn, M R; Welch, M J; Dence, C S; Tewson, T J; Saji, H; Maeda, M [Washington Univ., St. Louis, MO (USA). Edward Mallinckrodt Inst. of Radiology

    1984-07-01

    Syntheses of (/sup 18/F)haloperidol and (/sup 18/F)spiroperidol in both no-carrier-added and carrier-added forms have been accomplished. The no-carrier-added (/sup 18/F)butyrophenone neuroleptics were prepared in low (<2%) yield by acid decomposition of aryl piperidine triazenes. Carrier-added /sup 18/F-neuroleptics were prepared in better (5-17%) yields by /sup 18/F-for-/sup 19/F nucleophilic aromatic substitution. The preparation of all synthetic precursors, and procedures for radiolabeling are fully described.

  13. Electrochemical behaviour of some neuroleptics: Haloperidol and its derivatives.

    Science.gov (United States)

    Vire, J C; Fischer, M; Patriarche, G J; Christian, G D

    1981-05-01

    The electrochemical characteristics of Haloperidol and related compounds, representative neuroleptics of the butyrophenone family, have been investigated as a function of pH and concentration by direct-current, alternating-current and differential-pulse polarography and cyclic voltammetry at a hanging mercury drop electrode. A single cathodic wave representing an irreversible two-electron reduction is obtained, and its half-wave potential differs from that characteristic of aromatic ketone reduction. Adsorption processes disturb the wave behaviour and an adsorption prewave is observed at high concentrations. Quantitative measurements were successful in the concentration range 1 x 10(-4)-1 x 10(-6)M (0.4 mg/l.), the lower concentration representing the detection limit by differential-pulse polarography.

  14. Synthesis of N-methyl and N-11C-methyl spiperone by phase transfer catalysis in anhydrous solvent

    International Nuclear Information System (INIS)

    Omokawa, Hiroyoshi; Tanaka, Akira; Iio, Mayumi; Nishihara, Yoshiaki; Inoue, Osamu; Yamazaki, Toshio.

    1985-01-01

    Spiperone, a butyrophenone neuroleptic drug, has been used in binding studies of dopamine receptors. Langstrom et al. developed N- 11 C-methyl spiperone, and, in cooperate with Wagner et al., made it possible to visualize the distribution of dopamine receptors in the human brain in vivo. In this paper, we independently developed another synthetic method of N- 11 C-methyl spiperone using the phase transfer catalyst in an anhydrous solvent. Separation of the product is feasible only by passing the reactant solution through a Millipore filter and injecting it onto high pressure liquid chromatography (HPLC). The time required for the synthesis and purification of N- 11 C-methyl spiperone from 11 C-methyl iodide and spiperone was 20 min. Radiochemical yield exceeded 35 % against 11 C-methyl iodide without correcting decay of the radioactivity. (author)

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

    International Nuclear Information System (INIS)

    Rowell, F.J.; Hui, S.M.; Kamel, S.R.

    1981-01-01

    Radioimmunoassays for haloperidol are described, involving use of tritium-or 125 I-labeled drug or tritium-labeled spiroperidol, and a rabbit antiserum to a drug/bovine serum albumin conjugate. The 125 I-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)

    Rowell, F.J.; Hui, S.M.; Kamel, S.R.

    1981-01-01

    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. The neurotoxicity of pyridinium metabolites of haloperidol

    Directory of Open Access Journals (Sweden)

    Agnieszka Górska

    2015-10-01

    Full Text Available Haloperydol is a butyrophenone, typical neuroleptic agent characterized as a high antipsychotics effects in the treatment of schizophrenia and in palliative care to alleviation many syndromes, such as naursea, vomiting and delirium. Clinical problems occurs during and after administration of the drug are side effects, particularly extrapyrramidal symptoms (EPS. The neurotoxicity of haloperydol may be initiated by the cationic metabolites of haloperydol, HPP+, RHPP+, formed by oxidation and reduction pathways. These metabolites are transported by human organic cation transporters (hOCT to several brain structures for exapmle, in substantia nigra, striatum, caudate nucleus, hippocampus. After reaching the dopaminergic neurons inhibits mitochondrial complex I, evidence for free radical involvement, thus leading to neurodegeneration.

  18. Imaging dopamine transmission in schizophrenia

    International Nuclear Information System (INIS)

    Laruelle, M.

    1998-01-01

    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 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 2 receptor density parameters, under the assumption that all tracers labeled the same population of D 2 receptors. This analysis revealed that, compared to healthy controls, patients with schizophrenia present a significant but mild elevation of D 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 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

  19. Observational study of drug-drug interactions in oncological inpatients

    Directory of Open Access Journals (Sweden)

    María Sacramento Díaz-Carrasco

    2018-01-01

    Full Text Available Objective: To determine the prevalence of potential clinically relevant drug- drug interactions in adult oncological inpatients, as well as to describe the most frequent interactions. A standard database was used. Method: An observational, transversal, and descriptive study including patients admitted to the Oncology Service of a reference hospital. All prescriptions were collected twice a week during a month. They were analysed using Lexicomp® database, recording all interactions classified with a level of risk: C, D or X. Results: A total of 1 850 drug-drug interactions were detected in 218 treatments. The prevalence of treatments with at least one clinically relevant interaction was 95%, being 94.5% for those at level C and 26.1% for levels D and X. The drugs most commonly involved in the interactions detected were opioid analgesics, antipsychotics (butyrophenones, benzodiazepines, pyrazolones, glucocorticoids and heparins, whereas interactions with antineoplastics were minimal, highlighting those related to paclitaxel and between metamizole and various antineoplastics. Conclusions: The prevalence of clinically relevant drug-drug interactions rate was very high, highlighting the high risk percentage of them related to level of risk X. Due to the frequency of onset and potential severity, highlighted the concomitant use of central nervous system depressants drugs with risk of respiratory depression, the risk of onset of anticholinergic symptoms when combining morphine or haloperidol with butylscopolamine, ipratropium bromide or dexchlorpheniramine and the multiple interactions involving metamizole.

  20. Haloperidol Disrupts Opioid-Antinociceptive Tolerance and Physical Dependence

    Science.gov (United States)

    Yang, Cheng; Chen, Yan; Tang, Lei

    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 dependence by inhibiting CaMKII. The hypothesis was tested in two rodent models of opioid tolerance and dependence. Pretreatment with haloperidol (0.2–1.0 mg/kg i.p.) prevented the development of morphine tolerance and dependence in a dose-dependent manner. Short-term treatment with haloperidol (0.06–0.60 mg/kg i.p.) dose-dependently reversed the established morphine-antinociceptive tolerance and physical dependence. Correlating with behavioral effects, pretreatment or short-term treatment with haloperidol dose-dependently inhibited morphine-induced up-regulation of supraspinal and spinal CaMKIIα activity. Moreover, haloperidol given orally was also effective in attenuating morphine-induced CaMKIIα activity, antinociceptive tolerance, and physical dependence. Taken together, these data suggest that haloperidol attenuates opioid tolerance and dependence by suppressing CaMKII activity. Because haloperidol is a clinically used drug that can be taken orally, we propose that the drug may be of use in attenuating opioid tolerance and dependence. PMID:21436292

  1. Improved delineation of human dopamine receptors using [18F]-N-methylspiroperidol and PET

    International Nuclear Information System (INIS)

    Arnett, C.D.; Wolf, A.P.; Shiue, C.Y.; Fowler, J.S.; MacGregor, R.R.; Christman, D.R.; Smith, M.R.

    1986-01-01

    The brain uptake of [18F]-N-methylspiroperidol, a butyrophenone neuroleptic with high selectivity for the dopamine receptor, has been measured in three normal human volunteers using positron emission tomography for times up to 12 hr postinjection. These studies demonstrated two unique findings concerning the in vivo distribution of this neuroleptic: (a) it is tightly bound to dopamine D-2 receptors in the caudate-putamen brain regions, and (b) these regions are the only large brain structures which exhibit appreciable long-term retention. In addition, radioactivity clears rapidly from plasma, and the percentage of unchanged [18F]-N-methylspiroperidol in plasma declines rapidly. These results suggest that this compound binds irreversibly to dopamine D-2 receptors, and that there are few if any dopamine D-2 receptors in the human frontal cortex. These studies emphasize not only the importance of characterizing neurotransmitter receptors in living human brain using a ligand labeled with a positron emitting nuclide of sufficiently long half-life to allow monitoring of brain radioactivity distribution for several hours after the injection of radioligand, but also of accurately determining the amount of unchanged tracer in plasma for tracer kinetic modeling

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

    International Nuclear Information System (INIS)

    Larisch, R.; Klimke, A.

    1998-01-01

    The present review describes findings and clinical indications for the dopamine D 2 receptor scintigraphy. Methods for the examination of D 2 receptors are positron emission tomography (PET) using 11 C- or 18 F-labelled butyrophenones or benzamides or single photon emission tomography (SPECT) using 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 2 receptor binding (D 2 -RB) compared to control subjects. However, patients suffering from Steele-Richardson-Olszewski-Syndrome or Multiple System Atrophy show a decreased D 2 -RB and are generally non-responsive to treatment. Postsynaptic blockade of D 2 receptors results in a drug induced Parkinsonian syndrome, which can be diagnosed by D 2 scintigraphy. Further possible indications occur in psychiatry: The assessment of receptor occupancy is useful in schizophrenic patients treated with neuroleptics. Additionally, D 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 2 receptor binding can simplify the choice of therapy in depressive disorder: Patients showing a low D 2 binding are likely to improve following an antidepressive drug treatment whereas sleep deprivation is promising in patients with high D 2 binding. (orig.) [de

  3. Semi-Targeted Analysis of Complex Matrices by ESI FT-ICR MS or How an Experimental Bias may be Used as an Analytical Tool

    Science.gov (United States)

    Hertzog, Jasmine; Carré, Vincent; Dufour, Anthony; Aubriet, Frédéric

    2018-03-01

    Ammonia is well suited to favor deprotonation process in electrospray ionization mass spectrometry (ESI-MS) to increase the formation of [M - H]-. Nevertheless, NH3 may react with carbonyl compounds (aldehyde, ketone) and bias the composition description of the investigated sample. This is of significant importance in the study of complex mixture such as oil or bio-oil. To assess the ability of primary amines to form imines with carbonyl compounds during the ESI-MS process, two aldehydes (vanillin and cinnamaldehyde) and two ketones (butyrophenone and trihydroxyacetophenone) have been infused in an ESI source with ammonia and two different amines (aniline and 3-chloronaniline). The (+) ESI-MS analyses have demonstrated the formation of imine whatever the considered carbonyl compound and the used primary amine, the structure of which was extensively studied by tandem mass spectrometry. Thus, it has been established that the addition of ammonia, in the solution infused in an ESI source, may alter the composition description of a complex mixture and leads to misinterpretations due to the formation of imines. Nevertheless, this experimental bias can be used to identify the carbonyl compounds in a pyrolysis bio-oil. As we demonstrated, infusion of the bio-oil with 3-chloroaniline in ESI source leads to specifically derivatized carbonyl compounds. Thanks to their chlorine isotopic pattern and the high mass measurement accuracy, (+) ESI Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS) unambiguously highlighted them from the numerous CxHyOz bio-oil components. These results offer a new perspective into the detailed molecular structure of complex mixtures such as bio-oils. [Figure not available: see fulltext.

  4. New drug developments in the Latin Americas (Argentina, Costa Rica, Mexico and Panama).

    Science.gov (United States)

    Ban, T A; Galvan, L; Udabe, R U; Vergara, L; Zoch, C

    1974-07-01

    New drug developments in four Latin American countries, i.e. Argentina, Costa Rica, Mexico and Panama and the United States were compared. In contradistinction to the United States, clinical investigations with newly developed drugs in the four countries are based on contracts between individual investigators and the pharmaceutical industry without governmental interference. There are no adequate facilities to develop new psychoactive preparation in the four Latin American countries. Nevertheless, psychopharmacological practices are essentially the same as in the United States or Canada and all important psychoactive preparations used in the United States are available in the Latin Americas. Some of the newer-thioxanthene, butyrophenone and diphenylbutylpiperidine preparations which are still under clinical investigation in the United States are already available for clinical use in Argentina, Costa Rica, Mexico and Panama. While there is less governmental control than in the United States or Canada, with regard to clinical investigations of drugs or with regard to marketing newly developed preparations, there is no evidence of abuse. Finally, it should be noted that the introduction of psychotropic drugs brought about a new era in psychiatry in the Latin Americas. It becomes increasingly obvious that psychiatry today is practiced on the basis of knowledge derived from clinical impressions and on the basis of findings verified in clinical testings, i.e. on the basis of two different standards. Accordingly, as in Europe and North America, a re-examination of traditional concepts has begun in the Latin Americas. There are indications that biological psychiatry in general, and psychopharmacology in particular, are gaining increasing importance in the Latin Americas. This has led to the creation of a training program in biological psychiatry by the World Health Organization in Montreal, in cooperation with the Division of Psychopharmacology of the Department of

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

    International Nuclear Information System (INIS)

    Zanzonico, P.B.

    1982-01-01

    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- 11 C]-α-aminoisobutyric acid ([1- 11 C]-AIB), a transport system-specific radiotracer for tumor localization and for the assessment of amino acid transport in vivo; and [ 18 F]-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- 11 C]-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. [ 18 F]-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 [ 18 F]-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

  6. Prolactin releasing effect of sulpiride isomers in rats and man

    Energy Technology Data Exchange (ETDEWEB)

    Mueller, E E; Stefanini, E; Spano, P F [Cagliari Univ. (Italy). Inst. of Pharmacology and Pharmacognosy; Camanni, F; Massara, F [Turin Univ. (Italy). Chair of Endocrinology; Locatelli, V; Cocchi, D

    1979-01-01

    Sulpiride, an antipsychotropic drug of the benzamide class, reportedly displaces stereospecifically (/sup 3/H)-butyrophenones from putative dopamine (DA) binding sites in rat striatum. To evaluate if sulpiride displays the same stereospecifity in the inhibition of pituitary DA receptors, the effect of the two(-)-and (+)-sulpiride isomers was tested with regard to their ability to stimulate prolactin (PRL) secretion in rats and man and to displace (/sup 3/H)-spiroperidol bound to rat anterior pituitary receptors. In male rats, (-)-sulpiride at doses of 0.1 and 0.1 mg/kg i.p., induced a maximum PRL-releasing effect, not different from that evoked by a dose of 10 mg/kg of the compound. (+)-Sulpiride was active only at the dose of 10mg/kg i.p., and its PRL-releasing effect was superimposable to that evoked by the same dose of (-)-sulpiride. Similarily, in 8 normal subjects (4 men and 4 women) only (-)-sulpiride was active as PRL releaser when the low dose of 0.25 mg i.v. was used; when the higher dose of sulpiride was used (4.0 mg i.v.), it induced a rise in plasma PRL of the same entity for both isomers at early post-injection times (15-30 min) but greater with the (-)-isomer at the following time intervals (45-120 min). (-)-Sulpiride displaced (/sup 3/H)-spiroperidol bound to rat anterior pituitary homogenates with a potency about 100 times greater as that showed by (+)-sulpiride. In all, these data indicate that sulpiride isomers display at the level of pituitary DA receptors for PRL control the same stereospecifity exhibited on a population of striatal DA receptors.

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

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    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

  8. [No inhibition of intestinal motility following ketamine-midazolam anesthesia. A comparison of anesthesia with enflurane and fentanyl/midazolam].

    Science.gov (United States)

    Freye, E; Knüfermann, V

    1994-02-01

    weight. Also, the duration of operation was comparable in all three groups. Mean gastro-coecal transit time was 204 (+/- 19.6, SD) min following enflurane, 302 (+/- 32.8 SD) min following fentanyl/-midazolam and 210 (+/- 28.8 SD) min following ketamine/midazolam anaesthesia. The gastro-intestinal inhibition after the opioid-based anaesthetic technique was significantly prolonged (p constipation, is likely to develop postoperatively. In classical neuroleptanaesthesia and in analgosedation in the ICU, the simultaneous use of the butyrophenone droperidol seems to counteract the inhibition of opioid-related gastrointestinal motility. In cases of opioid-related gastrointestinal atonia a gastrokinetic compound may be necessary to overcome this effect on intestinal motility.

  9. Droperidol for acute psychosis.

    Science.gov (United States)

    Cure, S; Rathbone, J; Carpenter, S

    2004-10-18

    People suffering from acute psychotic illnesses, especially those associated with agitated or violent behaviour, may require urgent pharmacological tranquillisation or sedation. Droperidol, a butyrophenone neuroleptic, has been used for this purpose in several countries. To estimate the effects of droperidol compared to other treatments for controlling disturbed behaviour and reducing psychotic symptoms for people with suspected acute psychotic illnesses. We updated previous searches by searching the Cochrane Schizophrenia Group Register (September 2003). References of all identified studies were searched for further trial citations and authors of trials were contacted. Twenty-one other databases were also searched as part of a broader project and this composite database was searched for this review. This was supplemented by hand searching reference lists and contacting both the pharmacological industry and relevant authors. The review included randomised controlled trials comparing droperidol to any other treatment for people with suspected acute psychotic illnesses, including schizophrenia, schizoaffective disorder, mixed affective disorders, the manic phase of bipolar disorder or a brief psychotic episode. Relevant studies were selected for inclusion, their quality was assessed and data extracted. Data were excluded when more than 50% of participants were lost to follow up. For binary outcomes, standard estimates of risk ratio (RR) and the corresponding 95% confidence intervals (CI) were calculated. Where possible, weighted number needed to treat or harm statistics (NNT, NNH), and the corresponding 95% confidence intervals (CI), were calculated. We identified only two relevant trials. One additional study focused on outcomes at 30 days rather than at a few hours. One small (n = 41) randomised trial compared intravenous (iv) droperidol (10 mg) with iv placebo and found that people allocated to droperidol were significantly less likely to need additional

  10. [POISONING BY PSYCHOPHARMACOLOGICAL DRUGS IN AZERBAIJAN: THE RESULTS OF 8-YEAR PROSPECTIVE OBSERVATION].

    Science.gov (United States)

    Afandiyev, I; Azizov, V

    2017-11-01

    . Intoxication by serotonin reuptake inhibitors antidepressants, were relatively rare (3.8% of all cases of poisoning in T43). Among the poisonings with butyrophenone and thioxanthene neuroleptics, the first ranked place was occupied by cases of haloperidol poisoning, which accounted for 82.6% in this cohort. In the group of intoxications with other antipsychotic and neuroleptic drugs, the first ranked place belonged to the poisoning with clozapine - a total of 83 cases or 47.2% in cohort. Poisonings by psychopharmacological drugs occupy the first ranking place among poisoning by drugs, medicaments and biological substances (T36-T50). Increased control over the prescription and sale of psychopharmacological drugs, a reduction the number of tablets in one package, as well as increased attention to vulnerable groups of the population could be help to reduce the percentage of these poisonings in Azerbaijan.

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

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    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