β-肾上腺素能激动剂通过β1或β2受体降低自发运动活性。

Beta-adrenergic agonists reduce spontaneous motor activity through either beta 1 or beta 2 receptors.

作者信息

Frances H, Renwart N, Danti S, Cash R, Raisman R, Simon P

出版信息

Pharmacol Biochem Behav. 1987 Jan;26(1):11-5. doi: 10.1016/0091-3057(87)90525-9.

Abstract

In mice, the clenbuterol-induced decrease in spontaneous motor activity was antagonized by IPS-339 (beta 2 antagonist) but not by betaxolol (beta 1 antagonist), whereas the isoproterenol-induced decrease in spontaneous motor activity was completely antagonized by betaxolol and only partially by IPS-339. It can be concluded that the clenbuterol-induced decrease in spontaneous motor activity is of the beta 2-type, whereas that induced by isoproterenol is essentially of the beta 1 type. In addition, chronic treatment with clenbuterol induced a tachyphylaxis to the effect of clenbuterol but not of isoproterenol. After chronic administration of tricyclic antidepressants (imipramine and desipramine) the number of cortical beta 1 adrenergic receptors decreased without impairing the clenbuterol-induced decrease in spontaneous motor activity. We conclude that beta 2 adrenergic receptors mediate the clenbuterol-induced decrease in spontaneous motor activity and the tachyphylaxis to this effect after chronic treatment.

摘要

在小鼠中，克仑特罗诱导的自发运动活性降低被IPS - 339（β2拮抗剂）拮抗，但未被倍他洛尔（β1拮抗剂）拮抗，而异丙肾上腺素诱导的自发运动活性降低被倍他洛尔完全拮抗，仅被IPS - 339部分拮抗。可以得出结论，克仑特罗诱导的自发运动活性降低是β2型的，而异丙肾上腺素诱导的则主要是β1型的。此外，长期用克仑特罗治疗会导致对克仑特罗作用产生快速耐受性，但对异丙肾上腺素则不会。长期给予三环类抗抑郁药（丙咪嗪和地昔帕明）后，皮质β1肾上腺素能受体数量减少，但不影响克仑特罗诱导的自发运动活性降低。我们得出结论，β2肾上腺素能受体介导了克仑特罗诱导的自发运动活性降低以及长期治疗后对此作用的快速耐受性。