人类前列腺中的α - 1c肾上腺素受体:克隆、功能表达和定位到特定的前列腺细胞类型。
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曾曲克J, Kost T, Goetz A, Hazum S, Roberson KM, Haizlip J, Godinot N, Robertson CN, Saussy D
人类前列腺中的α - 1c肾上腺素受体:克隆、功能表达和定位到特定的前列腺细胞类型。
中国药物学杂志，1995年8月;115(8):1475-85。
- PubMed ID
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8564208 (PubMed视图］
- 摘要
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1.良性前列腺增生(BPH)导致老年男性尿路梗阻，经常需要手术来缓解尿潴留、夜尿和排尿症状。平滑肌张力，有助于扩大的腺体尿道收缩似乎是由- 1肾上腺素受体介导的。在这篇论文中，分子和药理学方法被用来建立在前列腺中发挥作用的α 1c肾上腺素能受体亚型。2.采用聚合酶链式反应(PCR)、Northern blot和原位杂交技术研究前列腺中α 1-肾上腺素能受体亚型的表达。前列腺间质细胞和腺细胞均表达α 1C亚型，腺细胞中表达α 1B和α 1D亚型。在前列腺癌组织间质和腺细胞中均观察到α 1C的高表达水平。3.从人前列腺中克隆了α 1c肾上腺素能受体cDNA。 Stable mammalian cell lines expressing human alpha 1B-, alpha 1C-, and alpha 1D-adrenoceptors were made. Membranes prepared from these cell lines and human prostate were used to evaluate the pharmacological profiles of human alpha 1B-, alpha 1C- and alpha 1D-adrenoceptors in comparison to human prostate. Leverage plot analysis of compound affinities determined by competition for [125I]-I-HEAT binding demonstrated that the alpha 1C subtype is the predominant alpha 1-adrenoceptor in human prostate. 4. The alpha 1-adrenoceptors cause smooth muscle constriction by coupling to IP3 turnover and intracellular Ca2+ release. Using stable cell lines to measure IP3 production in response to noradrenaline, alpha 1C stimulated IP3 production most efficiently, with alpha 1B at an intermediate level, while little IP3 above background could be detected with alpha 1D. These results supported a functional role of the alpha 1C-adrenoceptor on prostate smooth muscle constriction by noradrenaline stimulation.