Urapidil Analogues Are Potent Ligands of the 5-HT1A Receptor
| Autor: | G, Gross, K, Schüttler, X, Xin, G, Hanft |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Cerebral Cortex
Male Pharmacology 8-Hydroxy-2-(di-n-propylamino)tetralin Tetrahydronaphthalenes Adrenergic beta-Antagonists Rats Inbred Strains In Vitro Techniques Receptors Adrenergic alpha Ligands Piperazines Rats Receptors Serotonin Animals Guanosine Triphosphate Serotonin Antagonists Cardiology and Cardiovascular Medicine Adrenergic alpha-Antagonists |
| Zdroj: | Journal of Cardiovascular Pharmacology. 15:S8-S16 |
| ISSN: | 0160-2446 |
| DOI: | 10.1097/00005344-199001001-00003 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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