Romeo G, Russo F, Guccione S, Barbarulo D, De Blasi A
Istituto di Chimica Farmaceutica e Tossicologica, Catania.
Farmaco. 1995 Jun;50(6):471-7.
In the present paper recent results obtained in the field of the alpha 1-adrenoceptor (alpha 1AR) ligands are reported. Syntheses, alpha 1AR binding properties and structure-affinity relationships of tricyclic compounds containing the pyrimido-2,4-dione ring are described. Moreover, preliminary results on the binding properties of some derivatives for the recently cloned alpha 1AR subtypes expressed in COS-7 cells (alpha 1B, alpha 1C, alpha 1D) are discussed. Obtained data clearly indicate that some of the synthesized compounds are able to discriminate between the alpha 1B and the alpha 1C/alpha 1D adrenoceptor subclasses.
本文报道了在α1-肾上腺素能受体（α1AR）配体领域取得的最新成果。描述了含嘧啶-2,4-二酮环的三环化合物的合成、α1AR结合特性及结构-亲和力关系。此外，还讨论了一些衍生物对在COS-7细胞中表达的最近克隆的α1AR亚型（α1B、α1C、α1D）的结合特性的初步结果。所得数据清楚地表明，一些合成化合物能够区分α1B和α1C/α1D肾上腺素能受体亚类。
