Evidence for a complex interaction between the subtypes of the α1-adrenoceptor

Michael T. Piascik, Marta S. Sparks, Terry A. Pruitt, Edward E. Soltis

Research output: Contribution to journalArticlepeer-review

52 Scopus citations


Ligand binding studies with WB 4101 revealed that the rat aorta contains both the α1a- and α1b-adrenoceptor subtypes. Results obtained following treatment with the irreversible antagonists phenoxybenzamine, chlorethylclonidine or SZL-49 (4-amino-6,7-dimethoxy-2-quinazolinyl-4-(2-bicyclo[2,2,2]octa-2,5-dienylcarbonyl-2-piperazine) suggest that there is a complex interaction between the α1-adrenoceptor subtypes in the aorta. Chlorethylclonidine affects only the α1b-adrenoceptor, whereas the predominant action of SZL-49 is on the α1a-subtype. Chlorethylclonidine significantly inhibited the response to either methoxamine or phenylephrine, agents which are selective α1a-adrenoceptor agonists. Following inactivation with either chlorethylclonidine or SZL-49, the response of the rat aorta to phenylephrine was only partially antagonized by either prazosin or WB 4101. SZL-49 also inhibited the response of the rat tail artery to electrical stimulation. The response of the tail artery obtained following inactivation with SZL-49 was effectively antagonized by prazosin. Phenylephrine, prazosin or WB 4101 afforded complete protection from chlorethylclonidine adrenoceptor inactivation, while these same ligands were only partially effective against SZL-49. Either SZL-49 or chlorethylclonidine significantly impaired the irreversible adrenoceptor blocking actions of phenoxybenzamine. These results suggest: (1) only the α1a-adrenoceptor subtype appears to be associated with nerve terminals in the tail artery, (2) there may be a complex interaction between the α1-adrenoceptor subtypes such that both receptors must be iniact and functional to observe normal agonist and antagonist interactions, (3) there may be three sites of action for agonists associated with the rat aorta.

Original languageEnglish
Pages (from-to)279-289
Number of pages11
JournalEuropean Journal of Pharmacology
Issue number3
StatePublished - Jul 9 1991

Bibliographical note

Funding Information:
Supported in part by grants from the National Institutes of Health (HL-38120) and a grant-in-aidf rom the American Heart Association (to M.T.P.) and the American Heart Association-KentuckyA ffiliate (to E.E.S.).


  • Smooth muscle regulation (vascular)
  • α-Adrenoceptor subtypes
  • α-Adrenoceptors

ASJC Scopus subject areas

  • Pharmacology


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