药理特性的α1 a-adrenoceptor调停收缩在孤立的鼠尾动脉对去甲肾上腺素的反应。

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Lachnit工作组,Tran,克拉克·德·福特美联社

药理特性的α1 a-adrenoceptor调停收缩在孤立的鼠尾动脉对去甲肾上腺素的反应。

Br J杂志。1997年3月,120(5):819 - 26所示。

PubMed ID

9138687 (在PubMed

]

文摘

1。阿尔法1-adrenoceptor人口调停的鼠尾动脉收缩的特点是使用定量受体药理学。2。累积浓度效应(E /[一])曲线去甲肾上腺素(NA)产生了一个p[一]50 5.56 + / - 0.05 (n = 16)。哌唑嗪浓度引起的,平行,右旋E /(一)曲线转向收益率NA pKb 8.9(席尔德回归斜率= 1.0)。rs - 17053 (N - [2 - (2-cyclopropyl甲氧基苯氧基)乙基]5-chloro-alpha, alpha-dimethyl-1H-indole - 3-ethanamine盐酸盐;10 - 100海里),选择性α1 A-adrenoceptor拮抗剂,产生了非平行,两相的,右旋转变的E / NA(一)曲线,表明的参与多个α1-adrenoceptor亚型。高亲和力的分析组件产生一个明显的回目9.2 + / - 0.3的价值。3所示。- 61603,选择性受体激动剂在α1肾上腺素能受体的行为作为一个完整的受体激动剂相对于NA和产生单相E /(一)曲线的p (A50) 7.59 + / - 0.04 (n = 15)。 Pretreatment of tissues with chloroethylclonidine (CEC; 100 microM for 20 min, followed by 40 min washout), which preferentially alkylates alpha 1B- and alpha 1D-adrenoceptors, did not alter E/[A] curves to A-61603. Prazosin (3-300 nM) caused concentration-dependent, parallel, dextral shifts of E/[A] curves to A-61603 yielding a pA2 estimate of 9.2 +/- 0.2. 4. Experiments with alpha 1-adrenoceptor antagonists of varying subtype selectivities (RS-17053, SNAP 5089, tamsulosin, 5-methylurapidil, BMY 7378, HV 723 and REC 15/2739) revealed parallel dextral shifts of E/[A] curves to A-61603. Schild regression analyses yielded pA2 estimates of 9.2, 9.3, 11.2, 9.0, 6.3, 8.7 and 10.0 for RS-17053, SNAP 5089, tamsulosin, 5-methylurapidil, BMY 7378, HV 723 and REC 15/2739, respectively, although deviations from unit slope (possibly reflecting a secondary involvement of another alpha 1-adrenoceptor) hindered estimations of pKb for some antagonists. The antagonist affinity profile obtained reflects best that described for the alpha 1A-adrenoceptor. 5. In conclusion, caudal artery of rat contracts in response to NA via activation of at least two alpha 1-adrenoceptor subtypes. One of these subtypes displays the pharmacology of the alpha 1A-adrenoceptor, while the other remains to be defined. Use of the novel selective agonist, A-61603, allows for limited pharmacological isolation of the alpha 1A-adrenoceptor permitting characterization of the properties of selective antagonists.

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-1A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-1A肾上腺素能受体	蛋白质	人类	是的	受体激动剂	细节