中介的noradrenaline-induced收缩大鼠主动脉的α1 b-adrenoceptor亚型。

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把甲壳R,出的L, Poggesi E, Simonazzi我,塔代伊C, Leonardi

中介的noradrenaline-induced收缩大鼠主动脉的α1 b-adrenoceptor亚型。

Br J杂志。1995年2月,114 (4):745 - 50。

PubMed ID

7773533 (在PubMed

]

文摘

1。的亚型α1-adrenoceptor介导肿瘤收缩外源性去甲肾上腺素(NA)在大鼠主动脉检查生化和功能研究。2。培养的大鼠主动脉膜不可逆α1 b-adrenoceptor拮抗剂,chloroethylclonidine (CEC: 10 microM)并没有改变[3 h]哌唑嗪绑定的KD未经处理的膜相比,但减少了88%的总数结合位点(Bmax)。3所示。后的大鼠主动脉条收缩NA CEC (50 microM 30分钟)孵化其次是重复洗涤,表现出明显的转变在NA的效力和部分减少最大响应。NA CEC孵化后的残余收缩不受哌唑嗪(10海里)。4所示。竞争对手哌唑嗪、特拉唑嗪(R) ym - 12617,酚妥拉明,5-methylurapidil和spiperone抑制收缩NA估计pA2值为9.85,8.54,9.34,7.71,7.64和8.41,分别。5。 The affinity of the same antagonists for the alpha 1A- and alpha 1B- adrenoceptors was evaluated by utilizing membranes from rat hippocampus pretreated with CEC, and rat liver, respectively. 5-Methylurapidil and phentolamine were confirmed as selective for the alpha 1A-adrenoceptors, whereas spiperone was alpha 1B-selective. 6. A significant correlation was found between the pA2 values of the alpha 1-adrenoceptor antagonists tested and their affinity for the alpha 1B-adrenoceptor subtype, but not for the alpha 1A-subtype. 7. In conclusion, these findings indicate that in rat aorta most of the contraction is mediated by alpha 1B-adrenoceptors, and that the potency (pA2) of an antagonist in this tissue should be related to its antagonistic effect on this subtype of the alpha 1-adrenoceptor population.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Droxidopa	Alpha-1B肾上腺素能受体	蛋白质	人类	是的	受体激动剂	细节
去甲肾上腺素	Alpha-1B肾上腺素能受体	蛋白质	人类	是的	受体激动剂	细节