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牛乳头肌中3H-哌唑嗪与α1-肾上腺素能受体结合的鉴定与表征

Identification and characterization of 3H-prazosin binding to alpha 1-adrenoceptors in bovine teat muscles.

作者信息

Roets E, Peeters G

出版信息

Arch Int Pharmacodyn Ther. 1985 Jun;275(2):189-98.

PMID:2992402
Abstract

The highly specific alpha 1-adrenoceptor antagonist 3H-prazosin was used to characterize alpha 1-adrenoceptors in smooth muscles of the cistern wall of teats of lactating cows. Binding was rapid, readily reversible, stereospecific and saturable. Scatchard analysis of saturation binding data on bovine teat membranes revealed that 3H-prazosin bound to a single class (Bmax = 128 +/- 13 fmol/mg of membrane protein) of noncooperative sites (Hill coefficient = 0.95 +/- 0.02) with high affinity (KD = 0.47 +/- 0.05 nM). Competition binding studies with 9 antagonists and 8 agonists, indicated that 3H-prazosin labeled the alpha 1-receptor.

摘要

高特异性的α1-肾上腺素能受体拮抗剂3H-哌唑嗪被用于表征泌乳奶牛乳头乳池壁平滑肌中的α1-肾上腺素能受体。结合迅速、易于逆转、具有立体特异性且可饱和。对牛乳头膜饱和结合数据的Scatchard分析表明,3H-哌唑嗪与一类非协同位点(Bmax = 128 +/- 13 fmol/mg膜蛋白)结合,亲和力高(KD = 0.47 +/- 0.05 nM),希尔系数为0.95 +/- 0.02。用9种拮抗剂和8种激动剂进行的竞争结合研究表明,3H-哌唑嗪标记了α1受体。

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