Effects of (+/-)- (+)- and (-)-metoprolol, (+/-)- (+)- and (-)-pindolol, (+/-)-mepindolol and (+/-)-bopindolol on the rat left atria and portal vein.

General pharmacology Pub Date : 1991-01-01 DOI:10.1016/0306-3623(91)90597-y

S A Doggrell

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引用次数: 2

Abstract

1. The effects of (+/-)- (+)- and (-)-metoprolol, (+/-)- (+)- and (-)-pindolol, (+/-)-mepindolol and (+/-)-bopindolol on the beta 1-adrenoceptor mediated responses of the rat left atria and the beta 2-adrenoceptor mediated responses of the rat portal vein to isoprenaline have been determined. 2. Racemic and (-)-metoprolol were selective beta 1-adrenoceptor antagonists. (+)-Metoprolol was devoid of beta-adrenoceptor antagonistic activity. 3. Racemic and (-)-pindolol were potent and (+)-pindolol was a modest beta-adrenoceptor antagonist. 4. (+/-)-Mepindolol and (+/-)-bopindolol were apparently competitive antagonists of the isoprenaline beta 1-adrenoceptor mediated responses of the rat left atria but non-competitive antagonists of the isoprenaline beta 2-adrenoceptor mediated responses of the rat portal vein. 5. It is suggested that (+/-)-mepindolol and (+/-)-bopindolol are slowly dissociating beta-adrenoceptor antagonists and the non-competitive antagonism can only be detected on tissues with modest receptor reserves for maximum responses to isoprenaline.

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(+/-)-(+)-和(-)-美托洛尔，(+/-)-(+)-和(-)-品多洛尔，(+/-)-美品多洛尔和(+/-)-bopindolol对大鼠左心房和门静脉的影响。

1. 测定了(+/-)-(+)-(+)-和(-)-美托洛尔、(+/-)-(+)-和(-)-品多洛尔、(+/-)-美品多洛尔和(+/-)-bopindolol对大鼠左心房β 1-肾上腺素受体介导的反应和大鼠门静脉β 2-肾上腺素受体介导的异丙肾上腺素反应的影响。2. 外消旋和(-)-美托洛尔是选择性β 1-肾上腺素受体拮抗剂。(+)-美托洛尔缺乏-肾上腺素能受体拮抗活性。3.外消旋和(-)-pindolol是有效的，(+)-pindolol是一种适度的β -肾上腺素能受体拮抗剂。4. (+/-)-美品多洛尔和(+/-)-bopindolol是大鼠左心房异丙肾上腺素β 1-肾上腺素受体介导的竞争性拮抗剂，但对大鼠门静脉异丙肾上腺素β 2-肾上腺素受体介导的非竞争性拮抗剂。5. 这表明(+/-)-美平多洛尔和(+/-)-bopindolol是缓慢解离的β -肾上腺素受体拮抗剂，非竞争性拮抗剂只能在对异丙肾上腺素有最大反应的适度受体储备的组织中检测到。

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General pharmacology

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