BINDING PROFILE OF THE SELECTIVE MUSCARINIC RECEPTOR ANTAGONIST TRIPITRAMINE

被引：42

作者：

MAGGIO, R

BARBIER, P

BOLOGNESI, ML

MINARINI, A

TEDESCHI, D

MELCHIORRE, C

机构：

[1] UNIV BOLOGNA,DEPT PHARMACEUT SCI,I-40126 BOLOGNA,ITALY

[2] UNIV PISA,SCH MED,INST PHARMACOL,I-56100 PISA,ITALY

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1994年 / 268卷 / 03期

关键词：

TRIPITRAMINE; METHOCTRAMINE; MUSCARINIC RECEPTOR SUBTYPE; BINDING AFFINITY; CHO-K1; CELL;

D O I：

10.1016/0922-4106(94)90075-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The binding selectivity of the muscarinic antagonist tripitramine has been tested on the five cloned human muscarinic receptor subtypes (Hm(1) to Hm(5)) expressed in chinese hamster ovary (CHO-K1) cells. The results indicate that tripitramine binds to the muscarinic Hm(2) receptor with a K-i value of 0.027 +/- 0.02 nM. Tripitramine distinguishes Hm(2) vs. Hm(4) by a factor of 24 and vs. Hm(3) and Hm(5) by a factor of 142 and 125, respectively. A lower affinity ratio, about 6-fold, was found between muscarinic Hm(2) and Hm(1) receptors. A comparative study with the well-known selective muscarinic M(2) receptor antagonist methoctramine indicates that tripitramine has gained both potency and selectivity for the muscarinic Hm(2) receptor subtype.

引用

页码：459 / 462

页数：4

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