Conformational requirements of alpha2-adrenergic receptors

R. R. Ruffolo, K. S. Anderson, Duane Miller

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

The conformationally restrained trans-extended and cis-folded isomers of 2-(3,4-dihydroxyphenyl)cyclobutylamine were used to establish the conformational requirements of presynaptic alpha2-adrenergic receptors in the field-stimulated guinea pig ileum. The trans-extended isomer produced a concentration-dependent inhibition of the twitch response with an EC50 of 34 μM. The cis-folded analogue failed to produce a significant inhibition of the twitch response at concentrations up to 1 mM. These results suggest that the presynaptic alpha2-adrenergic receptor prefers phenethylamines in the trans-extended conformation over the cis-folded conformation. The conformational requirements of alpha1- and alpha2-adrenergic receptors appear to be similar.

Original languageEnglish (US)
Pages (from-to)259-261
Number of pages3
JournalMolecular Pharmacology
Volume21
Issue number2
StatePublished - 1982
Externally publishedYes

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Adrenergic Receptors
Phenethylamines
Ileum
Guinea Pigs

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Conformational requirements of alpha2-adrenergic receptors. / Ruffolo, R. R.; Anderson, K. S.; Miller, Duane.

In: Molecular Pharmacology, Vol. 21, No. 2, 1982, p. 259-261.

Research output: Contribution to journalArticle

Ruffolo, RR, Anderson, KS & Miller, D 1982, 'Conformational requirements of alpha2-adrenergic receptors', Molecular Pharmacology, vol. 21, no. 2, pp. 259-261.
Ruffolo, R. R. ; Anderson, K. S. ; Miller, Duane. / Conformational requirements of alpha2-adrenergic receptors. In: Molecular Pharmacology. 1982 ; Vol. 21, No. 2. pp. 259-261.
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