肾上腺素能受体,cholinoceptor-mediated机制监管的5 -羟色胺释放新生兔子的孤立的导管。

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肾上腺素能受体,cholinoceptor-mediated机制监管的5 -羟色胺释放新生兔子的孤立的导管。

Br J杂志。1996年9月,119 (1):91 - 8。

PubMed ID

8872361 (在PubMed

]

文摘

1。孤立的新生兔子的导管体外孵化和流出的5 -羟色胺(5 -)是由h.p.l.c.与电化学检测。此前提供的证据表明这五流出来源于神经内分泌气道黏膜上皮细胞(NEE)。2。去氧肾上腺素(1、10、30 microM)增强5 - 80的流出,分别为205%和290。5 -流出诱发10 microM苯肾上腺素不受毒素河豚毒素的存在(1 microM)。3所示。Rauwolscine,弧239(α肾上腺素受体(2 b)喜欢拮抗剂),育亨宾和哌唑嗪与10 microM苯肾上腺素浓度的方式的影响的IC50值150年,295年,分别为300和1700海里。之间的比率的比较(对手)的IC50值与Ki的相应比率值绑定的研究获得的α(2)-α(2 b),α(2 c) -和α肾上腺素受体亚型(2 d)强烈建议的参与一个α受体(2 b)。4所示。 5-HT outflow evoked by 10 microM phenylephrine was inhibited by 65% in the presence of 1 microM forskolin and abolished in the presence of 10 microM forskolin. 5. 5-HT outflow evoked by 10 microM phenylephrine was inhibited by about 45 and 70% in the presence of 0.1 and 1 microM isoprenaline, respectively. The inhibitory effect of 1 microM isoprenaline was only marginally antagonized by 1 microM, but blocked by 10 microM propranolol. 6. 5-HT outflow was not affected by the muscarine receptor agonist oxotremorine (10 microM), but was enhanced by 175% by 100 microM nicotine. The effect of nicotine was blocked by 100 microM hexamethonium and prevented by 1 microM tetrodotoxin or 1 microM yohimbine. 7. In conclusion, 5-HT release from NEE cells of the rabbit trachea is stimulated via alpha-adrenoceptors most likely of the alpha(2B)-subtype localized directly at the NEE cells. Activation of beta-adrenoceptors as well as direct activation of adenylyl cyclase by forskolin exert inhibitory effects on 5-HT release. Activation of nicotinic, but not of muscarinic receptors, also evokes the release of 5-HT. However, the effect of nicotine appears to be mediated indirectly via the release of noradrenaline.

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药物靶点

药物	目标	类	生物	药理作用	行动
育亨宾	Alpha-2B肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节