Tucker A L, Linden J, Robeva A S, D'Angelo D D, Lynch K R
Department of Biochemistry, University of Virginia, Charlottesville 22908.
FEBS Lett. 1992 Feb 3;297(1-2):107-11. doi: 10.1016/0014-5793(92)80338-h.
A bovine brain adenosine A1 receptor cDNA encoding a 326 amino acid protein has been identified. This cDNA, which encodes a protein greater than 90% identical to analogous rat and dog receptors, was transiently expressed in COS-1 cells. Recombinant receptors exhibited the features of bovine A1 receptors that distinguish it from rat and canine receptors, including subnanomolar Ki for 1,3-dipropyl-8-cyclopentylxanthine, R-phenylisopropyl- adenosine (R-PIA) and xanthine amino conjugate, and the distinct potency order: R-PIA greater than S-PIA much greater than 5'-N-ethylcarboxamidoadenosine greater than 2'-chloroadenosine. The results indicate that the pharmacological differences between A1 adenosine receptors among species result from only minor differences in receptor structures.
已鉴定出一种编码326个氨基酸蛋白质的牛脑腺苷A1受体cDNA。该cDNA编码的蛋白质与类似的大鼠和犬类受体有90%以上的同源性,并在COS-1细胞中瞬时表达。重组受体表现出牛A1受体区别于大鼠和犬类受体的特征,包括对1,3 - 二丙基 - 8 - 环戊基黄嘌呤、R - 苯异丙基腺苷(R - PIA)和黄嘌呤氨基共轭物的亚纳摩尔级Ki值,以及独特的效价顺序:R - PIA大于S - PIA远大于5'-N - 乙基羧酰胺腺苷大于2'-氯腺苷。结果表明,不同物种间A1腺苷受体的药理学差异仅源于受体结构的微小差异。