IMETIT AND N-METHYL DERIVATIVES - THE TRANSITION FROM POTENT AGONIST TO ANTAGONIST AT HISTAMINE H-3 RECEPTORS

被引：22

作者：

GANELLIN, CR ^{[1
]}

BANGANDERSEN, B ^{[1
]}

KHALAF, YS ^{[1
]}

TERTIUK, W ^{[1
]}

ARRANG, JM ^{[1
]}

GARBARG, M ^{[1
]}

LIGNEAU, X ^{[1
]}

ROULEAU, A ^{[1
]}

SCHWARTZ, JC ^{[1
]}

机构：

[1] INSERM,CTR PAUL BROCA,UNITE NEUROBIOL & PHARMACOL,F-75014 PARIS,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(00)80219-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Imetit {S-[2-(imidazol-4-yl)ethyl]isothiourea} is a potent H-3-agonist in vitro (on rat brain cortical slices; EC50 = 1 nM) and in vivo (ED50 approximately 1 mg/kg per os in mice). N-Methylimetit is also an agonist (EC50 = 15 nM) but dimethyl and trimethyl derivatives are antagonists (K(i) = 50 - 500 nM).

引用

页码：1231 / 1234

页数：4

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