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大鼠肾乳头中类风湿关节炎 - 腺苷受体的证实。

Demonstration of RA - adenosine receptors in rat renal papillae.

作者信息

Woodcock E A, Loxley R, Leung E, Johnston C I

出版信息

Biochem Biophys Res Commun. 1984 Jun 15;121(2):434-40. doi: 10.1016/0006-291x(84)90201-8.

Abstract

Adenylate cyclase in homogenates of rat renal papillae was stimulated by adenosine agonist compounds. Adenosine agonists neither stimulated nor inhibited cyclase activity in cortex or medulla. The rank order of agonist potencies was 5'N- ethylcarboxamide adenosine much greater than 2-chloroadenosine greater than L-N6-phenylisopropyladenosine = cyclohexyladenosine greater than D-N6-phenylisopropyladenosine. Stimulation of adenylate cyclase by 5'N- ethylcarboxamide adenosine was competitively antagonised by the methylxanthines, 1,3-diethyl-8- phenylxanthine and 8-phenyltheophylline; 1,3-diethyl-8- phenylxanthine being approximately 10 times more potent than 8-phenyltheophylline. These results demonstrate adenosine receptors of the RA-type localized to the papilla of the rat kidney.

摘要

大鼠肾乳头匀浆中的腺苷酸环化酶受到腺苷激动剂化合物的刺激。腺苷激动剂对皮质或髓质中的环化酶活性既无刺激作用也无抑制作用。激动剂效力的排序为:5'-N-乙基甲酰胺腺苷远大于2-氯腺苷大于L-N6-苯基异丙基腺苷=环己基腺苷大于D-N6-苯基异丙基腺苷。5'-N-乙基甲酰胺腺苷对腺苷酸环化酶的刺激作用被甲基黄嘌呤、1,3-二乙基-8-苯基黄嘌呤和8-苯基茶碱竞争性拮抗;1,3-二乙基-8-苯基黄嘌呤的效力约为8-苯基茶碱的10倍。这些结果表明,RA型腺苷受体定位于大鼠肾脏的乳头。

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