Affinities of Histamine H1-Antagonists in Guinea Pig Brain: Similarity of Values Determined from [3H]Mepyramine Binding and from Inhibition of a Functional Response |
| |
Authors: | S J Hill P Daum J M Young |
| |
Institution: | Department of Pharmacology, University of Cambridge, Cambridge, United Kingdom |
| |
Abstract: | Affinity constants for five antagonists at histamine H1-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 H1-receptors. The affinity constants obtained were similar to those determined on peripheral H1-receptors and from inhibition of high-affinity 3H]mepyramine binding. This provides strong evidence that at least some of the 3H]mepyramine binding sites in guinea pig brain can be identified with functional H1-receptors. |
| |
Keywords: | Histamine H -Receptors Cyclic AMP Adenosine Cerebral cortex Antagonist affinities |
本文献已被 PubMed 等数据库收录! |