PMID: 2869414Dec 1, 1985

Binding of agonists and antagonists to beta-adrenoceptors in rat vas deferens: relationship to functional response

Naunyn-Schmiedeberg's Archives of Pharmacology
J M MayK P Minneman

Abstract

The properties of beta-adrenoceptors in rat vas deferens were examined using radioligand binding assays of 125I-pindolol(125IPIN) and inhibition of electrically-evoked contractions of vas deferens in vitro. 125IPIN labelled a single class of high affinity binding sites with apparently mass action kinetics in membrane preparations of vas deferens with properties consistent with an essentially homogeneous population of beta 2-adrenoceptors. Isoprenaline inhibited electrically evoked (60 V, 1.0 ms, 0.1 Hz) contractions of vas deferens with an EC50 of 18.0 +/- 2.1 nM. KB values for antagonists in competitively antagonizing this response correlated well (r2 = 0.99) with the KD values for inhibition of 125IPIN binding. Inhibition of 125IPIN binding by isoprenaline, adrenaline, noradrenaline and salbutamol was determined under conditions designed to produce high and low affinity agonist binding. In the presence of 10 mM MgCl2, agonists inhibited specific 125IPIN binding with a relatively high potency and low Hill slope, while in the presence of 154 mM NaCl and 300 microM guanosine-5'-triphosphate, agonists inhibited specific 125IPIN binding with a lower potency and an apparent Hill slope closer to 1. To determine which affinity state ...Continue Reading

References

May 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·T HagaA G Gilman
Dec 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·W L TerasakiG Brooker
Sep 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·E M Ross, A G Gilman
Dec 5, 1980·European Journal of Pharmacology·V J LottiP Kling
Jul 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·J PithaS P Baker
Feb 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·L E LimbirdR J Lefkowitz
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

Citations

Mar 18, 1986·European Journal of Pharmacology·J M MayK P Minneman
Jul 26, 2005·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Hideo HondaM Kondo

Related Concepts

M-75
Adrenergic beta-Agonists
Adrenergic beta-Antagonists
Proventil
Aptina
Metazoa
Novodrin
Visken
Beta-adrenergic receptor
Vas Deferens Structure

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