RO 5-4864和PK 11195对豚鼠气管的作用。

Effects of RO 5-4864 and PK 11195 on guinea pig trachea.

作者信息

Matera M G, Costantino M, D'agostino B, Marabese I, Lucarelli C, Rossi F

机构信息

Institute of Pharmacology and Toxicology, Faculty of Medicine and Surgery-2nd University of Naples, Italy.

出版信息

Res Commun Mol Pathol Pharmacol. 1995 Dec;90(3):321-31.

PMID:8746480

Abstract

Previous reports have suggested a role played by peripheral benzodiazepine receptors (PBZ) in the regulation of calcium. The aid of this investigation was to evaluate the effects of Ro 5-4864 (PBZ agonist) and PK11195 (PBZ antagonist) in guinea pig trachea and their possible role in the regulation of calcium. Ro 5-4864 and PK 11195 showed spasmolytic effects on the contraction curve induced by acetylcholine. Moreover, Ro 5-4864, PK 11195 and diltiazem (a Ca2+ -antagonistic drug) shifted to the right the contraction curves induced by acetylcholine, potassium chloride (KCl), calcium chloride (CaCl2), or by Bay K 8644. These results demonstrate that the benzodiazepines and their antagonists may exhibit Ca2+ -antagonistic activity. Ro 5-4864 and PK 11195 may exert this effect at a site that is a component of, or is associated with, voltage operated calcium channels (VOC).

摘要

先前的报告表明外周苯二氮䓬受体（PBZ）在钙调节中发挥作用。本研究的目的是评估Ro 5-4864（PBZ激动剂）和PK11195（PBZ拮抗剂）对豚鼠气管的影响及其在钙调节中的可能作用。Ro 5-4864和PK 11195对乙酰胆碱诱导的收缩曲线表现出解痉作用。此外，Ro 5-4864、PK 11195和地尔硫䓬（一种Ca2+拮抗剂）使乙酰胆碱、氯化钾（KCl）、氯化钙（CaCl2）或Bay K 8644诱导的收缩曲线右移。这些结果表明苯二氮䓬类药物及其拮抗剂可能表现出Ca2+拮抗活性。Ro 5-4864和PK 11195可能在作为电压门控钙通道（VOC）的一个组成部分或与之相关的位点发挥这种作用。