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Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding.

Publication ,  Journal Article
Williams, LT; Lefkowitz, RJ
Published in: Science
May 21, 1976

A radioactively labeled alpha-adrenergic antagonist, [3H]dihydroergocryptine, binds specifically to a site on rabbit uterine membranes. Binding is rapid, reaching equilibrium in less than 17 minutes at 25 degrees C. Adrenergic agonists compete for this binding site with an order of affinities identical to the pharmacological potency order of these agents as alpha-adrenergic agonists (epinephrine greater than norepinephrine greater than isoprotereonl). The (-) stereoisomers of epinephrine and norepinephrine are 30 times more potent in competing for the site than the corresponding (+) stereoisomers. alpha-Adrenergic antagonists, such as phentolamine and phenoxybenzamine, potently compete for the binding sites while the beta-adrenergic antagonist propranolol does not. Structural analogs of catecholamines that are devoid of alpha-adrenergic physiological activity do not compete for [3H]dihydroergocryptine binding sites. These data suggest that alpha-adrenergic receptors can be directly identified and studied by [3H]dihydroergocryptine binding.

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Published In

Science

DOI

ISSN

0036-8075

Publication Date

May 21, 1976

Volume

192

Issue

4241

Start / End Page

791 / 793

Location

United States

Related Subject Headings

  • Uterus
  • Stereoisomerism
  • Receptors, Adrenergic
  • Rabbits
  • Propranolol
  • Kinetics
  • General Science & Technology
  • Female
  • Ergoloid Mesylates
  • Dopamine
 

Citation

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Williams, L. T., & Lefkowitz, R. J. (1976). Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding. Science, 192(4241), 791–793. https://doi.org/10.1126/science.4894
Williams, L. T., and R. J. Lefkowitz. “Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding.Science 192, no. 4241 (May 21, 1976): 791–93. https://doi.org/10.1126/science.4894.
Williams LT, Lefkowitz RJ. Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding. Science. 1976 May 21;192(4241):791–3.
Williams, L. T., and R. J. Lefkowitz. “Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding.Science, vol. 192, no. 4241, May 1976, pp. 791–93. Pubmed, doi:10.1126/science.4894.
Williams LT, Lefkowitz RJ. Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding. Science. 1976 May 21;192(4241):791–793.
Journal cover image

Published In

Science

DOI

ISSN

0036-8075

Publication Date

May 21, 1976

Volume

192

Issue

4241

Start / End Page

791 / 793

Location

United States

Related Subject Headings

  • Uterus
  • Stereoisomerism
  • Receptors, Adrenergic
  • Rabbits
  • Propranolol
  • Kinetics
  • General Science & Technology
  • Female
  • Ergoloid Mesylates
  • Dopamine