Literature DB >> 2996968

Is there a basis for distinguishing two types of P2-purinoceptor?

G Burnstock, C Kennedy.   

Abstract

It is suggested that the P2-purinoceptor may be separated into two subtypes largely on the basis of the rank order of agonist potency of structural analogues of ATP and also on the activity of antagonists at the P2-purinoceptor: Subtype 1 (designated P2X), potency order: alpha, beta-methyleneATP, beta, gamma-methyleneATP greater than ATP = 2 methylthioATP; antagonism by ANAPP3 and selectively desensitisation following administration of alpha, beta-methyleneATP; present in the vas deferens and urinary bladder of guinea-pig and rat, frog and rat ventricle, and also in the smooth muscle of the rat femoral artery and rabbit central ear artery, where they mediate excitation. Subtype 2 (designated P2Y), potency order: 2-methylthioATP much greater than ATP greater than alpha, beta-methyleneATP, beta, gamma-methyleneATP; weak antagonism by ANAPP3 and desensitisation following administration of alpha, beta-methyleneATP; present in the guinea-pig taenia coli and the longitudinal muscle layer of the rabbit portal vein, where they mediate relaxation and also on the vascular endothelial cells of the rat femoral artery and pig aorta (where occupation leads to the production of endothelium-derived relaxing factor). Differences in the structure of the P2-purinoceptor in various tissues may be useful in the development of drugs for the treatment of vascular, gastrointestinal and urinoglenital disorders.

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Year:  1985        PMID: 2996968     DOI: 10.1016/0306-3623(85)90001-1

Source DB:  PubMed          Journal:  Gen Pharmacol        ISSN: 0306-3623


  406 in total

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4.  The fade of the purinergic neurogenic contraction of the guinea-pig vas deferens: analysis of possible mechanisms.

Authors:  B Driessen; I von Kügelgen; R Bültmann; D B Elrick; T C Cunnane; K Starke
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5.  Inhibition by nucleotides acting at presynaptic P2-receptors of sympathetic neuro-effector transmission in the mouse isolated vas deferens.

Authors:  I von Kügelgen; E Schöffel; K Starke
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Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-11       Impact factor: 3.000

7.  Comparison between sympathetic adrenergic and purinergic transmission in the dog mesenteric artery.

Authors:  I Muramatsu; T Ohmura; M Oshita
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8.  Characterization of purinoceptors mediating depolarization of rat isolated vagus nerve.

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9.  Effects of pyrimidines on the guinea-pig coronary vasculature.

Authors:  A J Vials; G Burnstock
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10.  Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

Authors:  Sean Conroy; Nicholas D Kindon; Jacqueline Glenn; Leigh A Stoddart; Richard J Lewis; Stephen J Hill; Barrie Kellam; Michael J Stocks
Journal:  J Med Chem       Date:  2018-03-28       Impact factor: 7.446

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