Evidence for two atypical conformations of beta-adrenoceptors and their interaction with Gi proteins

European Journal of Pharmacology
I N SantosRegina C Spadari-Bratfisch

Abstract

In this study, we investigated whether the responses of right atria from sinoaortic denervated rats to CGP12177 (4(3-t-butylamino-2-hydroxypropoxy benzidimidazole-2 one, hydrochloride)), isoprenaline and norepinephrine desensitized in parallel and whether CGP12177 interacted with distinct conformations of beta-adrenoceptors. Right atria from rats 48 h after sinoaortic denervation were subsensitive to isoprenaline, norepinephrine and CGP12177. One week after sinoaortic denervation, the sensitivity to CGP12177 had recovered whereas the responses to isoprenaline and norepinephrine were still subsensitive, suggesting that the binding sites for these molecules showed independent behavior. In atria from 48 h sinoaortic-denervated rats, propranolol or 3 microM CGP20712A (2-hydroxy-5(2-((2-hydroxy-3-(4-((methyl-4-trifluormethyl)1H imidazole-2-yl)-phenoxypropyl) amino) ethoxy)-benzamide monomethane sulphonate)) blocked the responses to 10 nM-1 microM CGP12177 and steepened the curves. The concentration-response curves to CGP12177 in the presence of ICI118,551 (erythro-DL-1(-methylindan-4-yloxy)-3-isopropylamino-butan-2-ol) were biphasic, suggesting that CGP12177 interacted with at least two conformations of beta-adrenoceptors that showe...Continue Reading

References

Aug 1, 1989·Trends in Pharmacological Sciences·A J Kaumann
Sep 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·E N JubergP W Abel
Oct 14, 1986·European Journal of Pharmacology·D J DooleyN C Reymann
Nov 1, 1970·British Journal of Pharmacology·L L Iversen, P J Salt
Jun 1, 1995·Trends in Pharmacological Sciences·T Kenakin
Jan 1, 1996·Journal of Receptor and Signal Transduction Research·M D Pak, P H Fishman
Aug 1, 1996·British Journal of Pharmacology·A J Kaumann, P Molenaar
Jun 1, 1997·Naunyn-Schmiedeberg's Archives of Pharmacology·A J Kaumann, P Molenaar
Sep 25, 1999·Naunyn-Schmiedeberg's Archives of Pharmacology·M D LoweA J Kaumann
Jun 19, 2001·Canadian Journal of Physiology and Pharmacology·I N Santos, R C Spadari-Bratfisch
May 15, 2002·European Journal of Pharmacology·Jonathan R S Arch
Sep 19, 2002·British Journal of Pharmacology·Jillian G BakerStephen J Hill
May 31, 2003·Canadian Journal of Physiology and Pharmacology·I N SantosR C Spadari-Bratfisch
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Dec 1, 1964·Circulation Research·E M KRIEGER

❮ Previous
Next ❯

Citations

Jan 6, 2009·Annals of the New York Academy of Sciences·Regina C Spadari-Bratfisch, Iraides Nunes dos Santos
Dec 18, 2013·Nitric Oxide : Biology and Chemistry·Amarylis Claudine Bonito Azeredo WanschelMarta Helena Krieger
Aug 10, 2006·Stress : the International Journal on the Biology of Stress·Iraídes N Santos, Regina C Spadari-Bratfisch
May 22, 2007·Stress : the International Journal on the Biology of Stress·O KrizanovaL Kubovcakova

❮ Previous
Next ❯

Related Concepts

Related Feeds

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.