Cloning and functional characterization of a human Al adenosine receptor

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Abstract

A human brain hippocampus cDNA library was screened by hybridization with a dog Al adenosine receptor cDNA probe. Sequencing of the resulting clones identified a 978 residue open reading frame encoding a 326 amino acid polypeptide showing 95.7% similarity with the dog Al adenosine receptor. Individual clones of stably transfected CHO cells expressing the human Al receptor were obtained and tested for their response to the Al agonist CPA [N6-cyclopentyladenosine] in the presence of forskolin. One clone was further characterized with respect to membrane binding of various adenosine agonists and antagonists. The rank order of affinities observed was typical of an A1 adenosine receptor. A Kd value of 2.28 nM was determined using [3H]DPCPX [dipropylcyclopentyl-xanthine], an Al selective antagonist.

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    Copyright © 1992 Published by Elsevier Inc.