α1 a-adrenoceptor-mediated人类输精管的收缩反应。

文章的细节

引用

复制到剪贴板

古河道K,罗萨里奥DJ,史密斯DJ, Chapple CR、中山教授T, Chess-Williams R

α1 a-adrenoceptor-mediated人类输精管的收缩反应。

Br J杂志。1995年9月,116 (1):1605 - 10。

PubMed ID

8564226 (在PubMed

]

文摘

1。主要α1-adrenoceptor调解人类输精管的收缩为特征的体外利用亚型选择性拮抗剂。2。反应人类附睾的输精管得到苯肾上腺素胺摄取抑制剂的存在和普萘洛尔。α的影响1-adrenoceptor拮抗剂、5-methylurapidil oxymetazoline, WB4101,哌唑嗪和chloroethylclonidine检查和l型钙通道阻滞剂,硝苯地平。3所示。5-Methylurapidil、WB4101 oxymetazoline和哌唑嗪作为竞争对手对去甲肾上腺素的反应,产生的回目的值8.8,分别为9.2、7.7和8.8。所有四个对手产生席尔德情节与团结和类似边坡最大对去甲肾上腺素的反应并没有改变在任何对手面前。4所示。Tamsulosin(1纳米)向右移去甲肾上腺素量效曲线引起的收益率明显pKB值为10.0。 However, maximum responses were also reduced by 51% with this concentration of antagonist. 5. Incubation of tissues with chloroethylclonidine (100 microM for 40 min) failed to alter responses significantly but the presence of nifedipine (1 microM) reduced maximum responses to phenylephrine by 32%. 6. The high affinity of 5-methylurapidil, oxymetazoline and WB4101, together with the failure of chloroethylclonidine to antagonize responses, indicate that the predominant alpha 1-adrenoceptor mediating contraction of the human vas deferens has the characteristics previously described for the pharmacologically-defined alpha 1A-adrenoceptor. The data are also consistent with those described for the cloned alpha 1c-adrenoceptor subtype thereby supporting the hypothesis that the two receptors are identical. The human vas deferens therefore represents a readily accessible preparation for functional studies of the human alpha 1A-adrenoceptor.

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
Oxymetazoline	Alpha-1A肾上腺素能受体	蛋白质	人类	是的	部分激动剂	细节