立体选择性的猪该项莱克多巴胺的受体立体异构体。

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米尔斯,Kissel J,比德韦尔CA,史密斯DJ

立体选择性的猪该项莱克多巴胺的受体立体异构体。

J动物科学。2003年1月,81 (1):122 - 9。

PubMed ID

12597381 (在PubMed

]

文摘

盐酸莱克多巴胺是一种该项受体((betaAR)配体被批准用于猪提高胴体贫瘠。莱克多巴胺是产生商业四个立体异构体的混合物(RR, RS、SR、SS)。为了确定哪些立体异构体是活跃在猪以及他们是否表现出betaAR亚型选择性,受体亲和力和腺苷酸环化酶激活测定使用克隆猪beta1——beta2AR表示在中国仓鼠卵巢(CHO)细胞。离解常数(Kd)是由竞争决定位移莱克多巴胺[125 i] iodocyanopindolol绑定的立体异构体。RR异构体亲和力最高beta1——和betaAR (Kd分别为29日和26海里)。离解常数的立体异构体高(RS = 463和78海里,SR = 3230和831海里,党卫军= 16600和3530 nM beta1 beta2AR,分别)相对于RR立体异构体。异丙肾上腺素刺激腺苷酸环化酶活性相对于基底利率600% CHO细胞,无论betaAR亚型。莱克多巴胺立体异构体不显著(P > 0.05)通过beta1AR刺激腺苷酸环化酶在温和的附近(Kd)或高(10 (4)M)浓度。相比之下,RR异构体腺苷酸环化酶活动增加300%到200相对于基底利率通过beta2AR温和和hiconcentrations;SR立体异构体腺苷酸环化酶活动增加近100%。 Neither the RS nor SS stereoisomers were effective in activating adenylyl cyclase activity through the beta2AR. A pattern of stereoselective activation similar to that for adenylyl cyclase also was exhibited for lipolysis using porcine adipocytes. The RR stereoisomer was equal to isoproterenol in stimulating lipolysis, whereas the SR isomer was 50% as effective; the RS and SR stereoisomers did not stimulate lipolysis in porcine adipocytes. The porcine betaAR exhibited stereoselectivity toward ractopamine stereoisomers with the RR isomer exhibiting the highest affinity for the (beta1- and beta2AR. In contrast, ractopamine stereoisomers seemed to be more effective at eliciting adenosine cyclic 3',5'-phosphate responses from beta2AR than beta1AR. The RR isomer ilikely the functional stereoisomer of ractopamine, but its effectiveness may be compromised by the presence of competing isomers, in particular the RS stereoisomer.

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莱克多巴胺