Differential photoaffinity labelling of serotonin‐S2 receptors and histamine‐H1 receptors using 7‐azidoketanserin

FEBS Letters

Wouters, Walter¹  Leysen, Josée E.¹  Van Dun, Jacky¹  Laduron, Pierre M.¹ 

[1] Department of Biochemical Pharmacology, Janssen Pharmaceutics, B-2340 Beerse, Belgium

关键词: 7-Azidoketanserin;    Photoaffinity labeling;    Serotonin-S2 receptor;    Histamine-H1 receptor;    [3H]Spiperone;    [3H] Pyrilamine;   

DOI  :  10.1016/0014-5793(85)80318-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

7-Azidoketanserin, a potent photoaffinity probe for serotonin-S₂ receptors was shown to irreversibly photoinactivate histamine-H₁receptors as well. The photolabelling of H₁-receptors could be prevented by several selective histamine-H₁ antagonists. In guinea pig cerebellum, a brain area that is highly enriched in H₁-receptors, photolabelling could be directed exclusively to these receptors by adding a high concentration of pipamperone, which selectively blocks serotonin-S₂ receptors. In rat pre-frontal corex, a region that is enriched in serotonin-S₂ receptors, pyrilamine was used to block H₁-receptors, thereby directing the photolabelling exclusively to S₂-receptors.

【 授权许可】

Unknown