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犬隐静脉突触后α肾上腺素能受体的药理学分化

Pharmacological differentiation of postsynaptic alpha adrenoceptors in the dog saphenous vein.

作者信息

Fowler P J, Grous M, Price W, Matthews W D

出版信息

J Pharmacol Exp Ther. 1984 Jun;229(3):712-8.

PMID:6327969
Abstract

The dog saphenous vein has postsynaptic subpopulations of both alpha-1 and alpha-2 adrenoceptors which are easily demonstrable using selective agonists and antagonists. Specific alpha-1 (methoxamine and SK&F 89748) or mixed alpha-1, alpha-2 (l-norepinephrine and M7) agonists as well as the specific alpha-2 agonist, BHT 920, cause concentration-related contraction of this tissue. However, maximum contractions produced by alpha-2 activation are significantly less than maximum contractions produced by alpha-1 or combined alpha-1, alpha-2 adrenoceptor activation. SK&F 89748-induced contractions are competitively inhibited by prazosin (pA2 = 7.74) and rauwolscine (pA2 = 6.63); BHT 920-induced contractions are unaffected by prazosin but inhibited by rauwolscine (pA2 = 8.93). Contractile responses to l-norepinephrine are inhibited by prazosin, rauwolscine or phenoxybenzamine in a manner that suggests that norepinephrine interacts with two subtypes of alpha adrenoceptors in this tissue. These data indicate that the dog saphenous vein strip is a suitable in vitro preparation for study of drug action at both postsynaptic adrenoceptors inasmuch as either subpopulation of alpha adrenoceptor can be studied independently using specific agonists or antagonists.

摘要

犬隐静脉具有α-1和α-2肾上腺素能受体的突触后亚群,使用选择性激动剂和拮抗剂很容易证实这一点。特异性α-1(甲氧明和SK&F 89748)或混合α-1、α-2(左旋去甲肾上腺素和M7)激动剂以及特异性α-2激动剂BHT 920,可引起该组织浓度相关的收缩。然而,α-2激活产生的最大收缩明显小于α-1或联合α-1、α-2肾上腺素能受体激活产生的最大收缩。SK&F 89748诱导的收缩被哌唑嗪(pA2 = 7.74)和萝芙辛(pA2 = 6.63)竞争性抑制;BHT 920诱导的收缩不受哌唑嗪影响,但被萝芙辛抑制(pA2 = 8.93)。对左旋去甲肾上腺素的收缩反应被哌唑嗪、萝芙辛或酚苄明抑制,这表明去甲肾上腺素在该组织中与两种α肾上腺素能受体亚型相互作用。这些数据表明,犬隐静脉条是研究药物对突触后肾上腺素能受体作用的合适体外制剂,因为可以使用特异性激动剂或拮抗剂独立研究α肾上腺素能受体的任一亚群。

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