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

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Abstract
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.