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输卵管供血动脉中突触后α-肾上腺素能受体的特性

Characterization of postsynaptic alpha-adrenoceptors in the arteries supplying the oviduct.

作者信息

Costa G, Isla M, García-Pascual A, Jimenez E, Recio P, Labadia A, García-Sacristán A

机构信息

Departamento de Fisiología, Facultad de Veterinaria, Universidad Complutense, Madrid, Spain.

出版信息

Br J Pharmacol. 1992 Feb;105(2):381-7. doi: 10.1111/j.1476-5381.1992.tb14262.x.

Abstract
  1. In vitro experiments were designed to characterize postjunctional alpha-adrenoceptor subtypes in ring segments (1 mm length; outer diameter 300-500 microns) from arteries supplying the oviduct of the heifer. 2. Noradrenaline, adrenaline and phenylephrine evoked concentration-dependent contractile responses. The pD2 values were 5.67, 5.89 and 5.93, respectively. Medetomidine clonidine and B-HT 920 (2-amino-6-allyl-5,6,7,8-tetra-hydro-4H-(thiazo)-4,5-d-azepoine ) were ineffective. 3. The alpha-adrenoceptor selective antagonists, prazosin (1 nM-0.1 microM) and rauwolscine (0.1-10 microM) competitively antagonized the response to noradrenaline. The pA2 values were 9.38 and 6.83, respectively. 4. The dissociation constant (KD) for noradrenaline calculated by use of the irreversible antagonist, dibenamine, was 3.95 (2.09-5.81) microM. The occupancy-response relationship was non-linear. Half-maximal response to noradrenaline was obtained with 22% receptor occupancy while maximal response required 100% occupancy. 5. B-HT 920 evoked a biphasic contractile concentration-dependent response in preparations incubated in a physiological solution containing 20 mM K+, 0.1 microM prazosin and 1 microM propranolol. Rauwolscine 0.1 microM significantly (P less than 0.01) blocked the first component of the B-HT 920 concentration-response curve with an apparent pA2 value of 8.52 (7.86-9.18). 6. These results strongly suggest that alpha-adrenoceptors in oviductal arteries are mainly of the alpha 1 subtype, although a possible role for alpha 2-adrenoceptors cannot be excluded.
摘要
  1. 设计体外实验以表征来自小母牛输卵管供血动脉的环形节段(长度1毫米;外径300 - 500微米)中的节后α - 肾上腺素能受体亚型。2. 去甲肾上腺素、肾上腺素和苯肾上腺素引发浓度依赖性收缩反应。pD2值分别为5.67、5.89和5.93。美托咪定、可乐定和B - HT 920(2 - 氨基 - 6 - 烯丙基 - 5,6,7,8 - 四氢 - 4H -(噻唑)- 4,5 - 二氮杂卓)无效。3. α - 肾上腺素能受体选择性拮抗剂哌唑嗪(1 nM - 0.1 μM)和育亨宾(0.1 - 10 μM)竞争性拮抗对去甲肾上腺素的反应。pA2值分别为9.38和6.83。4. 使用不可逆拮抗剂双苄胺计算的去甲肾上腺素解离常数(KD)为3.95(2.09 - 5.81)μM。占有率 - 反应关系是非线性的。去甲肾上腺素的半数最大反应在受体占有率为22%时获得,而最大反应需要100%占有率。5. 在含有20 mM钾、0.1 μM哌唑嗪和1 μM普萘洛尔的生理溶液中孵育的制剂中,B - HT 920引发双相收缩浓度依赖性反应。0.1 μM育亨宾显著(P小于0.01)阻断B - HT 920浓度 - 反应曲线的第一成分,表观pA2值为8.52(7.86 - 9.18)。6. 这些结果强烈表明,输卵管动脉中的α - 肾上腺素能受体主要是α1亚型,尽管不能排除α2 - 肾上腺素能受体的可能作用。

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