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扎考必利，一种强效的5-羟色胺3拮抗剂。

Zacopride, a potent 5-HT3 antagonist.

作者信息

Smith W W, Sancilio L F, Owera-Atepo J B, Naylor R J, Lambert L

机构信息

Department of Pharmacology, A. H. Robins Co., Richmond, VA 23220.

出版信息

J Pharm Pharmacol. 1988 Apr;40(4):301-2. doi: 10.1111/j.2042-7158.1988.tb05253.x.

DOI:10.1111/j.2042-7158.1988.tb05253.x
PMID:2900319
Abstract

The substituted benzamide derivative zacopride was found to antagonize competitively the effects of 5-hydroxytryptamine (5-HT) on the guinea-pig ileum, the rabbit vagus nerve and the von Bezold Jarisch reflex in the rat. The potency of zacopride was comparable with that of ICS 205-930 and it is concluded that zacopride possesses 5-HT3 receptor antagonizing properties.

摘要

已发现取代苯甲酰胺衍生物扎考必利能竞争性拮抗5-羟色胺（5-HT）对豚鼠回肠、兔迷走神经及大鼠贝佐尔德-雅里什反射的作用。扎考必利的效价与ICS 205-930相当，由此得出结论，扎考必利具有5-HT3受体拮抗特性。

相似文献

1
Zacopride, a potent 5-HT3 antagonist.扎考必利，一种强效的5-羟色胺3拮抗剂。
J Pharm Pharmacol. 1988 Apr;40(4):301-2. doi: 10.1111/j.2042-7158.1988.tb05253.x.
2
Comparison of the 5-HT3 receptor antagonist properties of ICS 205-930, GR38032F and zacopride.ICS 205-930、GR38032F和扎考必利对5-羟色胺3受体的拮抗特性比较。
J Pharmacol Exp Ther. 1989 Jan;248(1):197-201.
3
The enantiomers of zacopride: an intra-species comparison of their potencies in functional and anxiolytic models.扎考必利的对映体：在功能和抗焦虑模型中种内效价比较
Br J Pharmacol. 1995 Jul;115(5):775-80. doi: 10.1111/j.1476-5381.1995.tb15000.x.
4
Use of stereoisomers of zacopride to analyze actions of 5-hydroxytryptamine on enteric neurons.使用扎考必利的立体异构体来分析5-羟色胺对肠神经元的作用。
Am J Physiol. 1991 Jan;260(1 Pt 1):G80-90. doi: 10.1152/ajpgi.1991.260.1.G80.
5
Zacopride: anxiolytic profile in rodent and primate models of anxiety.扎考必利：在啮齿动物和灵长类动物焦虑模型中的抗焦虑特性
J Pharm Pharmacol. 1988 Apr;40(4):302-5. doi: 10.1111/j.2042-7158.1988.tb05254.x.
6
Comparison of potencies of 5-HT3 receptor antagonists at inhibiting aversive behavior to illumination and the von Bezold-Jarisch reflex in the mouse.5-羟色胺3（5-HT3）受体拮抗剂对抑制小鼠光照厌恶行为和贝佐尔德-雅里什反射的效能比较
Neuropharmacology. 1994 Feb;33(2):227-34. doi: 10.1016/0028-3908(94)90013-2.
7
Emetic activity of zacopride in ferrets and its antagonism by pharmacological agents.扎考必利在雪貂中的催吐活性及其被药物的拮抗作用。
Eur J Pharmacol. 1990 Jun 8;181(3):303-6. doi: 10.1016/0014-2999(90)90094-m.
8
The (S)-isomer of [3H]zacopride labels 5-HT3 receptors with high affinity in rat brain.[3H]扎考必利的（S）-异构体在大鼠脑中以高亲和力标记5-HT3受体。
Eur J Pharmacol. 1990 Jun 8;181(3):283-7. doi: 10.1016/0014-2999(90)90090-s.
9
5-HT3 receptor agonism may be responsible for the emetic effects of zacopride in the ferret.5-羟色胺3受体激动作用可能是扎考必利在雪貂中致吐作用的原因。
Br J Pharmacol. 1991 May;103(1):1011-2. doi: 10.1111/j.1476-5381.1991.tb12292.x.
10
LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity.马来酸LY277359：一种强效且选择性的5-羟色胺3受体拮抗剂，无促胃肠动力活性。
J Pharmacol Exp Ther. 1990 Jul;254(1):350-5.

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