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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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1
Pharmacological differentiation of postsynaptic alpha adrenoceptors in the dog saphenous vein.犬隐静脉突触后α肾上腺素能受体的药理学分化
J Pharmacol Exp Ther. 1984 Jun;229(3):712-8.
2
Insights into the unusual alpha adrenoceptor subtype in dog saphenous vein using phenoxybenzamine.利用酚苄明探究犬隐静脉中异常的α肾上腺素能受体亚型
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Postsynaptic alpha adrenoceptors on vascular smooth muscle.血管平滑肌上的突触后α肾上腺素能受体。
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Role of extracellular calcium in contractions produced by activation of postsynaptic alpha-2 adrenoceptors in the canine saphenous vein.细胞外钙在犬隐静脉突触后α-2肾上腺素能受体激活所产生收缩中的作用。
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Unusual alpha-adrenoceptor subtype in canine saphenous vein: comparison to mesenteric vein.犬隐静脉中异常的α-肾上腺素能受体亚型:与肠系膜静脉的比较。
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J Pharmacol Exp Ther. 1988 Jan;244(1):206-12.

引用本文的文献

1
Differential contributions of alpha-1 and alpha-2 adrenoceptors to vasoconstriction in mesenteric arteries and veins of normal and hypertensive mice.α-1和α-2肾上腺素能受体对正常和高血压小鼠肠系膜动脉和静脉血管收缩的不同作用。
Vascul Pharmacol. 2007 May;46(5):373-82. doi: 10.1016/j.vph.2007.01.003. Epub 2007 Jan 27.
2
The effects of some alpha-adrenoceptor antagonists on the responses of the canine saphenous vein to B-HT 933, UK-14304 and methoxamine.
Naunyn Schmiedebergs Arch Pharmacol. 1987 Mar;335(3):261-8. doi: 10.1007/BF00172794.
3
The effectiveness of alpha 2-adrenoceptor activation increases from the distal to the proximal part of the veins of canine limbs.α2 -肾上腺素能受体激活的有效性从犬类肢体静脉的远端到近端逐渐增强。
Br J Pharmacol. 1990 Oct;101(2):387-93. doi: 10.1111/j.1476-5381.1990.tb12719.x.
4
Pharmacological subclassification of alpha 1-adrenoceptors in vascular smooth muscle.血管平滑肌中α1肾上腺素能受体的药理学亚分类
Br J Pharmacol. 1990 Jan;99(1):197-201. doi: 10.1111/j.1476-5381.1990.tb14678.x.
5
Alpha-adrenoceptor subtypes in dog saphenous vein that mediate contraction and inositol phosphate production.介导犬隐静脉收缩和肌醇磷酸生成的α-肾上腺素能受体亚型。
Br J Pharmacol. 1991 Jan;102(1):151-61. doi: 10.1111/j.1476-5381.1991.tb12146.x.
6
SK&F 104078, a post-junctionally selective alpha 2-adrenoceptor antagonist in the human saphenous vein in vitro.SK&F 104078,一种在体外人隐静脉中具有节后选择性的α2肾上腺素能受体拮抗剂。
Naunyn Schmiedebergs Arch Pharmacol. 1992 Mar;345(3):327-32. doi: 10.1007/BF00168694.