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. 1993 Jul;109(3):693–698. doi: 10.1111/j.1476-5381.1993.tb13629.x

Functional characterization of three adenosine receptor types

MF Gurden, J Coates, F Ellis, B Evans, M Foster, E Hornby, I Kennedy, DP Martin, P Strong, CJ Vardey, A Wheeldon
PMCID: PMC2175648  PMID: 8358566

Abstract

1 The purpose of the present study was to classify adenosine receptors into A1 and A2 subtypes in a wide range of isolated tissues and cell types (rat adipocytes and atria, guinea-pig ileum and atria (A1); guinea-pig aorta, dog coronary artery and human platelets and neutrophils (A2)) using the R- and S-diastereoisomers of N-phenylisopropyladenosine (PIA), N-cyclopentyladenosine (CPA), the novel compound, N-[(1S,trans)-2-hydroxycyclopentyl]adenosine (GR79236), N-[(2-methylphenyl)methyl]adenosine (metrifudil), 2-(phenylamino)adenosine (CV1808), and 2-[[2-[4-(2-carboxyethyl)phenyl]ethyl]amino]-N-ethylcarboxamidoadenosine (CGS21680); N-ethylcarboxamidoadenosine (NECA) was used as a standard.

2 Results obtained in all tissue preparations previously reported to contain A1-receptors could be described by a single rank order of agonist potency: CPA ≥ GR79236, R-PIA ≥ NECA >> S-PIA ≥ metrifudil ≥ CV1808, CGS21680.

3 In contrast, two distinct rank orders of agonist potency were observed in preparations previously reported to contain A2-receptors. In dog coronary artery, human neutrophils and platelets the rank order of potency was: CV1808, CGS21680 ≥ NECA > R-PIA ≥ metrifudil ≥ CPA > GR79236, S-PIA. However, in guinea-pig aorta the rank order was: NECA > metrifudil > R-PIA, CPA > CV1808, GR79236 ≥ S-PIA, CGS21680.

4 The results of this study are consistent with the existence of three types of adenosine receptor: A1-and two subtypes of A2-receptor. The receptor present in dog coronary artery, human platelets and neutrophils, probably corresponds to the A2a subtype, whilst that present in the guinea-pig aorta may be of the A2b subtype.

Keywords: Adenosine receptors; A1, A2; GR79236; metrifudil; P1-purinoceptors

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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