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肾上腺素能激动剂对有色家兔眼内压及睫状体腺苷酸环化酶活性的影响。

The effects of adrenergic agonists on intraocular pressure and on adenylyl cyclase activity of ciliary processes in pigmented rabbits.

作者信息

Cepelík J, Dedina M, Hynie S

机构信息

Institute of Pharmacology, First Faculty of Medicine, Charles University, Prague, Czech Republic.

出版信息

Physiol Res. 1998;47(1):53-60.

PMID:9708702
Abstract

The effects of beta-adrenergic agonists isoprenaline, fenoterol and clenbuterol on the activity of adenylyl cyclase from ciliary processes and on intraocular pressure were examined in pigmented rabbits. Isoprenaline, fenoterol and clenbuterol stimulated adenylyl cyclase activity in vitro, but clenbuterol behaved as a partial agonist. Preincubation of ciliary processes with any of these three drugs led to the heterologous desensitization of adenylyl cyclase to the stimulatory effects of beta-adrenergic agonists or vasoactive intestinal peptide (VIP). This desensitization was dose-dependent and was expressed mainly as a decrease of the highest effects of stimulatory drugs. The exact mechanism of this phenomenon is not yet known. After topical administration, all three tested beta-adrenergic agonists decreased intraocular pressure with approximately the same intensity. The relationship between ocular hypotensive effects of beta-adrenergic agonists and their effects on adenylyl cyclase of ciliary processes is discussed. It is concluded that ocular hypotensive effects of adrenergic agonists and other drugs stimulating adenylyl cyclase cannot be explained simply by stimulation or desensitization of adenylyl cyclase of ciliary processes.

摘要

在有色家兔中研究了β-肾上腺素能激动剂异丙肾上腺素、非诺特罗和克仑特罗对睫状体腺苷酸环化酶活性及眼压的影响。异丙肾上腺素、非诺特罗和克仑特罗在体外刺激腺苷酸环化酶活性,但克仑特罗表现为部分激动剂。用这三种药物中的任何一种对睫状体进行预孵育,都会导致腺苷酸环化酶对β-肾上腺素能激动剂或血管活性肠肽(VIP)的刺激作用产生异源脱敏。这种脱敏是剂量依赖性的,主要表现为刺激药物的最大效应降低。这一现象的确切机制尚不清楚。局部给药后,所有三种受试β-肾上腺素能激动剂均以大致相同的强度降低眼压。讨论了β-肾上腺素能激动剂的降眼压作用与其对睫状体腺苷酸环化酶作用之间的关系。得出的结论是,肾上腺素能激动剂和其他刺激腺苷酸环化酶的药物的降眼压作用不能简单地用睫状体腺苷酸环化酶的刺激或脱敏来解释。

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