New analogues of oxotremorine and oxotremorine-M - Estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes

被引：21

作者：

Barocelli, E

Ballabeni, V

Bertoni, S

Dallanoce, C

De Amici, M

De Micheli, C

Impicciatore, M

机构：

[1] Univ Parma, Ist Farmacol & Farmacognosia, I-43100 Parma, Italy

[2] Univ Milan, Ist Chim Farmaceut & Tossicol, I-20131 Milan, Italy

来源：

LIFE SCIENCES | 2000年 / 67卷 / 06期

关键词：

muscarinic agonists; oxotremorine; functional determination of affinity and efficacy;

D O I：

10.1016/S0024-3205(00)00661-5

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Two subsets of tertiary amines (1a-6a) and methiodides (1b-6b) with a structural resemblance to oxotremorine and oxotremorine-M were tested at rabbit vas deferens (M-1), guinea pig left atrium (M-2), guinea pig ileum and urinary bladder (M-3) muscarinic receptor subtypes, The pharmacological profile of the derivatives under study has been discussed by evaluating their potency, affinity and efficacy as well as the regional differences in muscarinic receptor occupancy. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：717 / 723

页数：7

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