Pharmacologic characterization of cloned α1-adrenoceptor subtypes: selective antagonists suggest the existence of a fourth subtype

Debra A. Schwinn*, Jon W. Lomasney

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

97 Scopus citations

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 languageEnglish (US)
Pages (from-to)433-436
Number of pages4
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume227
Issue number4
DOIs
StatePublished - Dec 1 1992

Keywords

  • Adrenoceptors
  • Catecholamines
  • Inositol phosphates

ASJC Scopus subject areas

  • Pharmacology

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