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豚鼠心室肌细胞不存在A2腺苷受体的证据。

Evidence against the presence of A2 adenosine receptors on guinea pig ventricular myocytes.

作者信息

Wilken A, Tawfik-Schlieper H, Schwabe U

机构信息

Pharmakologisches Institut, Universität Heidelberg, F.R.G.

出版信息

Eur J Pharmacol. 1991 Jan 3;192(1):161-3. doi: 10.1016/0014-2999(91)90083-3.

Abstract

The effects of different adenosine agonists on cAMP levels in isolated adult guinea pig ventricular myocytes were investigated. 2-Chloro-N6-cyclopentyladenosine (CCPA), R-N6-phenylisopropyl-adenosine (R-PIA), S-N6-phenylisopropyladenosine (S-PIA) and 5'-N-ethylcarboxamidoadenosine (NECA) reduced isoprenaline-stimulated cAMP Both the nonselective adenosine antagonist 8-[4-[( [[(2-aminoethyl)amino]carbonyl]methyl)oxy]-phenyl]-1, 3-dipropylxanthine ('xanthine amine congener'; XAC) and the A1-selective adenosine antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) blocked the inhibitory effect of NECA. Basal cAMP levels were not altered by NECA or the highly A2-selective 2-[p-(2-carboxyethyl)phenethylamino]-5'-N-ethylcarboxamidoadenosin e (CGS 21680), either alone or in the presence of DPCPX or XAC. These results provide evidence against the existence of A2 receptors on the ventricular myocyte but support the presence of A1 receptors.

摘要

研究了不同腺苷激动剂对成年豚鼠离体心室肌细胞中环磷酸腺苷(cAMP)水平的影响。2-氯-N6-环戊基腺苷(CCPA)、R-N6-苯异丙基腺苷(R-PIA)、S-N6-苯异丙基腺苷(S-PIA)和5'-N-乙基羧酰胺腺苷(NECA)均可降低异丙肾上腺素刺激的cAMP水平。非选择性腺苷拮抗剂8-[4-[( [[(2-氨基乙基)氨基]羰基]甲基)氧基]-苯基]-1,3-二丙基黄嘌呤(“黄嘌呤胺同类物”;XAC)和A1选择性腺苷拮抗剂8-环戊基-1,3-二丙基黄嘌呤(DPCPX)均能阻断NECA的抑制作用。单独使用或在DPCPX或XAC存在的情况下,NECA或高A2选择性的2-[对-(2-羧乙基)苯乙氨基]-5'-N-乙基羧酰胺腺苷(CGS 21680)均未改变基础cAMP水平。这些结果提供了反对心室肌细胞上存在A2受体的证据,但支持A1受体的存在。

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