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Differential photoaffinity labelling of serotonin‐S2 receptors and histamine‐H 1 receptors using 7‐azidoketanserin
Author(s) -
Wouters Walter,
Van Dun Jacky,
Leysen Josée E.,
Laduron Pierre M.
Publication year - 1985
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(85)80318-5
Subject(s) - receptor , serotonin , pyrilamine , 5 ht receptor , 5 ht1 receptor , histamine , histamine h1 receptor , class c gpcr , photoaffinity labeling , histamine receptor , biology , chemistry , biochemistry , endocrinology , agonist , metabotropic receptor , antagonist
7‐Azidoketanserin, a potent photoaffinity probe for serotonin‐S 2 receptors was shown to irreversibly photoinactivate histamine‐H 1 receptors as well. The photolabelling of H 1 ‐receptors could be prevented by several selective histamine‐H 1 antagonists. In guinea pig cerebellum, a brain area that is highly enriched in H 1 ‐receptors, photolabelling could be directed exclusively to these receptors by adding a high concentration of pipamperone, which selectively blocks serotonin‐S 2 receptors. In rat pre‐frontal corex, a region that is enriched in serotonin‐S 2 receptors, pyrilamine was used to block H 1 ‐receptors, thereby directing the photolabelling exclusively to S 2 ‐receptors.