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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. Regional localization of halopemide, a new psychotropic agent, in the rat brain

    NARCIS (Netherlands)

    Loonen, A.J.M.; Van Wijngaarden, I.; Janssen, P.A.J.; Soudijn, W.

    1978-01-01

    Halopemide is a new psychotropic agent, structurally related to the neuroleptics of the butyrophenone type, but with a different pharmacological and clinical profile. The concentration of halopemide in the rat brain is about 10 times less than that of R 29800, its chemical congener and of spiperone,

  4. Regional distribution of halopemide, a new psychotropic agent, in the rat brain at different time intervals and after chronic administration

    NARCIS (Netherlands)

    Loonen, A.J.M.; Van Wijngaarden, I.; Janssen, P.A.J.; Soudijn, W.

    1979-01-01

    Only a very small amount of halopemide, a new psychotropic agent, structurally related to the butyrophenones, but with a different pharmacological and clinical profile, penetrates into the rat brain. The maximum concentration is reached between 1 and 2 hours after injection. Halopemide is evenly dis

  5. Antipsychotic agents and QT changes.

    OpenAIRE

    Welch, R.; Chue, P

    2000-01-01

    Recently, antipsychotic medications of the novel or atypical classes have received increased attention because of concerns with respect to potential lengthening of the QT interval, yet the currently available and commonly prescribed conventional antipsychotics are significantly more cardiotoxic, particularly agents in the butyrophenone and phenothiazine classes. Lengthening of the QT interval can be associated with a fatal paroxysmal ventricular arrhythmia known as torsades de pointes. The sp...

  6. Accidental haloperidol poisoning in children

    Directory of Open Access Journals (Sweden)

    Mona P Gajre

    2012-01-01

    Full Text Available 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 parkinsonian symptoms. There are few case reports of accidental haloperidol poisoning in children and this one of them.

  7. [Chemotherapies of negative schizophrenia].

    Science.gov (United States)

    Petit, M; Dollfus, S

    1991-01-01

    Five years ago, Goldberg claimed that negative symptoms of schizophrenia do respond to neuroleptics. This apparent discovery is, in fact, a very common way of thinking for European schools of psychiatry, specially the French one guided by Delay and Deniker. Initially focused on reserpine and some alerting phenothiazines such as thioproperazine, this opinion has been extended to benzamides in the 1970s. The analysis of the publications devoted to this point indicates that several drugs are actually considered as potent disinhibitors (i.e. active on negative symptoms of schizophrenia): Phenothiazines: As shown in the controlled studies by Itil (1971), Poirier-Littré (1988), fluphenazine and pipotiazine improve the BPRS anergia factor and the SANS score. Butyrophenones: The first description of the "imipramine like" effect of trifluperidol by Janssen (1959) initiated the studies by Gallant (1960), Fox (1963). They compared trifluperidol at low doses versus haloperidol and chlorpromazine at medium and high doses, BPRS anergia factor improved only at low doses. Diphenylbutylpiperidines (DPBP): Meltzer's review (1986) concluded to the efficacy of such drugs on negative symptoms appearing as a specific biochemical relationship effect. A definite analysis about doses leads to a very different interpretation: DPBP low doses and only low doses improved negative symptoms as much as some low doses of phenothiazines. On the opposite, DPBP, phenothiazines and butyrophenones high doses are inefficient.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:1683624

  8. 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.)

  9. 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.

  10. [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

  11. 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.

  12. 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

  13. 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

  14. 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

  15. 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

  16. 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