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更新于：2025-05-07

1192U90

更新于：2025-05-07

概要

概要

基本信息

药物类型

小分子化药

别名-

靶点

5-HT1A receptor x 5-HT2 receptor x D2 receptor x D4 receptor

作用方式

激动剂、拮抗剂

作用机制

5-HT1A receptor激动剂(5-羟色胺1A受体激动剂)、5-HT2 receptor拮抗剂(5-羟色胺2受体拮抗剂)、D2 receptor拮抗剂(多巴胺D2受体拮抗剂)

+ [1]

治疗领域

其他疾病

在研适应症-

非在研适应症

精神分裂症

原研机构

GSK Plc

在研机构-

非在研机构

GSK Plc

权益机构-

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C22H27N5OS

InChIKeyGMDXHLCLNHCEIC-UHFFFAOYSA-N

CAS号155289-31-9

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关联

100 项与 1192U90 相关的临床结果

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100 项与 1192U90 相关的转化医学

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100 项与 1192U90 相关的专利（医药）

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项与 1192U90 相关的文献（医药）

1998-06-01·Bioorganic & Medicinal Chemistry3区 · 医学

Analogues of the potential antipsychotic agent 1192U90: amide modifications

3区 · 医学

Article

作者: Lee T. Schaller ; Frank Navas ; Mark H. Norman ; Flora L.M. Tang

Analogues of 2-amino-N-(4-(4-(1,2-benzisothiazol-3-yl)-l-piperazinyl) -butyl)benzamide hydrochloride (1192U90) were prepared and evaluated in receptor binding assays for the dopamine D2, serotonin 5-HT1a, and serotonin 5-HT2 receptors. Eight compounds have been synthesized in which the amide group of 1192U90 has been replaced with a variety of functional groups (i.e. ester, ketone, thioamide, butyramide, butyranilide, sulfonamide, alkoxyamide and hydrazide). These compounds exhibited moderate to potent affinities (0.55-200 nM) for all three receptors. Several analogues exhibited improved selectivity for the 5-HT2 receptor with D2/5-HT2 binding ratios greater than 1192U90.

1998-01-01·Journal of Chromatography A2区 · 化学

Use of liquid chromatography–tandem mass spectrometry for the quantitative and qualitative analysis of an antipsychotic agent and its metabolites in human plasma and urine

2区 · 化学

Article

作者: Gordon J Dear ; Stephen Pleasance ; Jeffrey Long ; Ian J Fraser ; Dipak K Patel

The use of liquid chromatography-tandem mass spectrometry (LC-MS-MS) for the quantitative analysis of an 'atypical' antipsychotic agent in human plasma is described. The method uses atmospheric pressure chemical ionisation, and offers increased sensitivity, selectivity and speed of analysis over an existing high-performance liquid chromatography method using fluorescence detection. This method enabled same day turn around of results for in excess of 100 samples, including sample preparation, data acquisition and processing. LC-MS-MS was also used to detect and characterise known and unknown in vivo metabolites of the drug in human urine and plasma, using electrospray ionisation.

1996-09-01·Toxicologic Pathology4区 · 医学

The Experimental Antipsychotic Agent 1192U90 Targets Tapetum Lucidum in Canine Eyes

4区 · 医学

Article

作者: Dykstra, Michael J. ; Dillberger, John E. ; O'Mara, Michael ; Peiffer, Robert L. ; Patel, Dipak K.

To assess the potential adverse effects in people of the antipsychotic agent 1192U90, we dosed mice, rats, beagles, and cynomolgus monkeys for up to 3 mo. In dogs, but not the other species, 1192U90 caused ocular changes detectable ophthalmoscopically as loss of tapetal reflectivity, altered tapetal color, and the appearance of black pigmentation on the tapetal fundus. Eyes from affected dogs had atrophic tapeta lucidum due to cell loss. Rodlets in remaining tapetal cells were separated by electron-lucent spaces or finely granular material, varied in size and shape, and often contained irregularly shaped electron-dense inclusions. Nontapetal ocular structures were unaffected. Because 1192U90 caused no ocular changes in nontapetal species, we hypothesized that it targeted only tapetum lucidum and spared other ocular structures. We tried to test this hypothesis by dosing congenitally atapetal dogs; however, although these dogs were ophthalmoscopically "atapetal," they had scattered tapetal cells visible by electron microscopy, and these tapetal cells had ultrastructural changes indistinguishable from those that occurred in treated normal-eyed dogs. Tapetal degeneration caused by 1192U90 resembled that described in hereditary tapetal degeneration in beagles. That 1192U90 caused no ocular changes in nontapetal species suggests that the ocular changes in dogs do not imply a risk for humans, whose eyes also lack a tapetum lucidum.

100 项与 1192U90 相关的药物交易

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