McBean D E, Harper A M, Rudolphi K A
Wellcome Surgical Institute, University of Glasgow, Scotland.
J Cereb Blood Flow Metab. 1988 Feb;8(1):40-5. doi: 10.1038/jcbfm.1988.6.
The aim of this study was to test the effect of adenosine and four of its analogues, 5'-(N-ethyl)carboxamidoadenosine (NECA), 2-chloroadenosine (2-CADO), L-phenylisopropyladenosine (L-PIA), and N6-cyclohexyl-adenosine (CHA), on prostaglandin (PG) F2 alpha-constricted pig basilar arteries, and from their rank order of potency determine the receptor type involved. The order of potency for the relaxation of the PGF2 alpha constriction was NECA greater than adenosine, 2-CADO greater than L-PIA greater than CHA, which is in keeping with the A2 receptor subtype. The study also investigated the effects of a known adenosine antagonist, namely, the xanthine derivative 8-phenyltheophylline, which at concentrations having no intrinsic effect (10(-8) and 10(-7) M) produced a significant shift to the right only for the NECA dose-response curve.
本研究的目的是测试腺苷及其四种类似物，即5'-(N-乙基)羧酰胺腺苷（NECA）、2-氯腺苷（2-CADO）、L-苯基异丙基腺苷（L-PIA）和N6-环己基腺苷（CHA），对前列腺素（PG）F2α收缩的猪基底动脉的作用，并根据它们的效价顺序确定所涉及的受体类型。PGF2α收缩舒张的效价顺序为NECA大于腺苷，2-CADO大于L-PIA大于CHA，这与A2受体亚型一致。该研究还调查了一种已知的腺苷拮抗剂，即黄嘌呤衍生物8-苯基茶碱的作用，其在无内在效应的浓度（10^(-8)和10^(-7) M）下仅使NECA剂量反应曲线显著右移。
