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

Science
L T Williams, Robert J Lefkowitz

Abstract

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.

References

Jan 1, 1984·Acta Biotheoretica·S C Brooks
Sep 1, 1984·Naunyn-Schmiedeberg's Archives of Pharmacology·A ClosseH J Tobler
Nov 15, 1978·Experientia·M Titeler, P Seeman
Sep 15, 1978·European Journal of Pharmacology·D C U'prichard, S H Snyder
Dec 9, 1983·European Journal of Pharmacology·A Davis
Oct 29, 1985·European Journal of Pharmacology·J P Maltier, C Legrand
Dec 15, 1976·Life Sciences·A Closse, D Hauser
Nov 15, 1977·Life Sciences·M S KafkaJ L Costa
Jan 1, 1979·Comparative Biochemistry and Physiology. C: Comparative Pharmacology·S A Kempson, G V Marinetti
Aug 1, 1979·Quarterly Reviews of Biophysics·J Giesecke, H Hebert
Jun 19, 1980·The New England Journal of Medicine·B Hoffman, Robert J Lefkowitz
Mar 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·L T WilliamsRobert J Lefkowitz
Sep 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·M TittlerP Seeman
Aug 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·B HoffmanJ N Fain
Nov 1, 1984·Biological Reviews of the Cambridge Philosophical Society·P H ReinhartF L Bygrave
Oct 1, 1977·The Journal of Clinical Investigation·L T Williams, Robert J Lefkowitz
Apr 3, 2008·The Journal of Clinical Investigation·Robert J Lefkowitz
Jan 1, 1982·Clinical and Experimental Hypertension. Part A, Theory and Practice·S J BlumenthalS G Iams
May 8, 2013·Angewandte Chemie·Robert J Lefkowitz
Feb 7, 1977·Biochemical and Biophysical Research Communications·T Ciaraldi, G V Marinetti
Aug 26, 1977·Brain Research·J N DavisR J Leefkowitz
Aug 15, 1979·Biochemical Pharmacology·M S Kafka, N B Thoa
Aug 1, 1989·British Journal of Pharmacology·W DuranteA K Sen
Jan 1, 1988·Fundamental & Clinical Pharmacology·J P Maltier, C Legrand
Mar 1, 1982·Journal of Autonomic Pharmacology·K G Digges
Mar 1, 1983·Clinics in Endocrinology and Metabolism·B Hoffman
Dec 9, 1977·Brain Research·D C U'prichardS H Snyder
Aug 3, 2013·Circulation Research·Elizabeth M McNally

Related Concepts

Molecular Stereochemistry
Tissue Membrane
Stereoisomers
Uterus
Analog
Catecholamines Measurement
Adrenergic Agonists
Adrenergic alpha-Agonists
Adrenergic alpha-Antagonists
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