Abstract
In membranes prepared from Cos-7 or HeLa cells expressing one of three individual cloned α1-adrenoceptor subtypes, competition with 2-{(β-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl}-tetralone ([125I]HEAT) by the selective compounds [+] niguldipine, 5-methyl-urapidil and benoxathian reveals high affinity for the clones α1-adrenoceptor subtype and low affinity for both the cloned α1A-adrenoceptor and α1B-adrenoceptor. Competition with [125I]HEAT by spiperone revealed high affinity for the cloned α1C-adrenoceptor, intermediate affinity for the cloned α1B-adrenoceptor, and low affinity for the cloned α1A-adrenoceptor. Combining pharmacological properties previously described for α1-adrenoceptor subtypes in rat membranes and here described from cloned receptors, these data suggest the existence of a fourth distinct α1-adrenoceptor subtype.
Original language | English (US) |
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Pages (from-to) | 433-436 |
Number of pages | 4 |
Journal | European Journal of Pharmacology: Molecular Pharmacology |
Volume | 227 |
Issue number | 4 |
DOIs | |
State | Published - Dec 1 1992 |
Keywords
- Adrenoceptors
- Catecholamines
- Inositol phosphates
ASJC Scopus subject areas
- Pharmacology