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Affinities of Histamine H 1 ‐Antagonists in Guinea Pig Brain: Similarity of Values Determined from [ 3 H]Mepyramine Binding and from Inhibition of a Functional Response
Author(s) -
Hill S. J.,
Daum P.,
Young J. M.
Publication year - 1981
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1981.tb04692.x
Subject(s) - mepyramine , histamine , histamine receptor , guinea pig , receptor , affinities , chemistry , binding site , stereochemistry , long term potentiation , biochemistry , biology , pharmacology , antagonist , endocrinology
Affinity constants for five antagonists at histamine H 1 ‐receptors in guinea pig brain have been determined from inhibition of the potentiation by histamine of the adenosine‐induced accumulation of cyclic AMP in cerebral cortical slices. This action of histamine appeared to be mediated solely through H 1 ‐receptors. The affinity constants obtained were similar to those determined on peripheral H 1 ‐receptors and from inhibition of high‐affinity [ 3 H]mepyramine binding. This provides strong evidence that at least some of the [ 3 H]mepyramine binding sites in guinea pig brain can be identified with functional H,‐receptors.