β-香树脂醇棕榈酸酯诱导活动减退的α-肾上腺素能受体介导机制。

An alpha-adrenoceptor-mediated mechanism of hypoactivity induced by beta-amyrin palmitate.

作者信息

Subarnas A, Tadano T, Kisara K, Ohizumi Y

机构信息

Pharmaceutical Institute, Tohoku University, Sendai, Japan.

出版信息

J Pharm Pharmacol. 1993 Nov;45(11):1006-8. doi: 10.1111/j.2042-7158.1993.tb05649.x.

DOI:10.1111/j.2042-7158.1993.tb05649.x

PMID:7908030

Abstract

Inhibitory effects of beta-amyrin palmitate in locomotor activity of mice were studied by combining this compound with alpha-adrenergic agonists or antagonists and a dopaminergic agonist. beta-Amyrin palmitate (2.5, 5.0 and 10.0 mg kg-1, i.p.) decreased locomotor activity of mice in a dose-dependent manner. It enhanced hypoactivity of mice treated with clonidine (0.025 mg kg-1, i.p.) and antagonized hyperactivity produced by phenylephrine (40 micrograms, i.c.v.). The inhibitory action of beta-amyrin palmitate was not affected by yohimbine (1.5 mg kg-1, i.p.), but was potentiated by prazosin (0.75 mg kg-1, i.p.). When combined with a dopaminergic agonist, apomorphine (2.0 mg kg-1, i.p.), beta-amyrin palmitate (5.0 and 10.0 mg kg-1, i.p.) did not affect locomotor stimulation produced by apomorphine. These results suggest that beta-amyrin palmitate might inhibit alpha 1-adrenoceptors.

摘要

通过将β-香树脂醇棕榈酸酯与α-肾上腺素能激动剂或拮抗剂以及多巴胺能激动剂联合使用，研究了其对小鼠自发活动的抑制作用。β-香树脂醇棕榈酸酯（2.5、5.0和10.0 mg kg-1，腹腔注射）以剂量依赖的方式降低了小鼠的自发活动。它增强了可乐定（0.025 mg kg-1，腹腔注射）处理的小鼠的活动减退，并拮抗了去氧肾上腺素（40微克，脑室内注射）引起的活动亢进。β-香树脂醇棕榈酸酯的抑制作用不受育亨宾（1.5 mg kg-1，腹腔注射）的影响，但被哌唑嗪（0.75 mg kg-1，腹腔注射）增强。当与多巴胺能激动剂阿扑吗啡（2.0 mg kg-1，腹腔注射）联合使用时，β-香树脂醇棕榈酸酯（5.0和10.0 mg kg-1，腹腔注射）不影响阿扑吗啡引起的运动兴奋。这些结果表明，β-香树脂醇棕榈酸酯可能抑制α1-肾上腺素能受体。