Urapidil analogues are potent ligands of the 5-HT1A receptor.
Urapidil and three derivatives with hypotensive properties (5-acetyl-, 5-formyl-, 5-methylurapidil) bind selectively to 5-HT receptors of the 5-HT1A subtype and to alpha 1-adrenoceptors labeled by [3H]8-OH-DPAT and [3H]prazosin, respectively. Binding to these receptors is likely to contribute to their hypotensive action. 5-Methylurapidil, the most potent of these drugs, was used in its 3H-labeled form as a radioligand. After blockade of alpha 1-adrenoceptors by prazosin, [3H]5-methylurapidil binds with nanomolar affinity to a binding site that is similar to the (5-HT1A) site labeled by [3H]8-OH-DPAT. No binding to other 5-HT1 and 5-HT2 receptors was observed. 5-HT uptake inhibitors did not inhibit [3H]5-methylurapidil binding. [3H]5-methylurapidil binding is sensitive to GTP and is modulated by divalent cations. Our results show that urapidil derivatives bind to the 5-HT1A recognition site and that [3H]5-methylurapidil is a valuable tool for the investigation of this receptor subtype.[1]References
- Urapidil analogues are potent ligands of the 5-HT1A receptor. Gross, G., Schüttler, K., Xin, X., Hanft, G. J. Cardiovasc. Pharmacol. (1990) [Pubmed]
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