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141374-81-4

中文名称 他折派特
英文名称 tarazepide
CAS 141374-81-4
分子式 C28H24N4O2
分子量 448.52
MOL 文件 141374-81-4.mol
141374-81-4 结构式 141374-81-4 结构式

基本信息

中文别名
他折派特
英文别名
tarazepide
4H-Pyrrolo[3,2,1-ij]quinoline-2-carboxamide, N-[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-5,6-dihydro-

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜

常见问题列表

生物活性
Tarazepide 是一种有效且特异性的 CCK-A 受体拮抗剂。
靶点

CCK-A receptor

体内研究

Tarazepide decreases duodenal electric activity, reduces interdigestive pancreatic secretion, especially protein; reduces cephalic and early postprandial (milk) induced secretion of bicarbonate and protein.Pancreatic protein secretion to intravenous CCK-8 was little affected by atropine, but was significantly reduced by Tarazepide±Atropine; in contrast, protein secretion to intraduodenal CCK-8 was abolished by Tarazepide or atropine. Leptin is administered to the animals at doses of 0.1, 1.0 or 10.0 μg/kg i.d. Tarazepide (2.5 mg/kg, i.d.), a CCK(1) receptor antagonist, is given to the rats prior to the application of leptin. CCK plasma level is measured by radioimmunoassay (RIA) following administration of leptin to the rats. Intraduodenal administration of leptin (1.0 or 10.0 microg/kg) to the fasted rats significantly and dose-dependently increases pancreatic protein and amylase outputs. Pancreatic secretory responses to leptin were totally abolished by prior capsaicin deactivation of sensory nerves or by pretreatment of the rats with Tarazepide.

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