PMID: 9416771Jan 1, 1997Paper

Chloroethylclonidine is a partial alpha1A-adrenoceptor agonist in cells expressing recombinant alpha1-adrenoceptor subtypes

Life Sciences
R Villalobos-MolinaJ A García-Sáinz

Abstract

Chloroethylclonidine increased cytosol [Ca2+] in rat-1 fibroblasts stably expressing alpha1a-adrenoceptors. The effect of the imidazoline was dose-dependent with a maximal effect (approximately 3-fold increase in [Ca2+]i) at 10 microM and it was blocked by phentolamine and 5-methyl urapidil, indicating that it was mediated through alpha1-adrenoceptors. Noradrenaline (1 microM) induced a much bigger effect (approximately 6-8-fold) in the same cells. When chloroethylclonidine was added before noradrenaline a dose-dependent inhibition of the effect of the natural catecholamine was observed. Chloroethylclonidine did not modified cytosol [Ca2+] in rat-1 fibroblast expressing alpha1b- or alpha1d-adrenoceptors. However, the imidazoline acutely inhibited the effect of noradrenaline in these cells. It is concluded that chloroethylclonidine interacts with alpha1a-adrenoceptors as a partial agonist inducing Ca2+ mobilization in a very short time frame and that it is able to inhibit the action of noradrenaline when co-incubated with the catecholamine in cells expressing any of the three alpha1-adrenoceptor subtypes.

References

Oct 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·S CotecchiaB K Kobilka
Sep 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·J P Nunes, S Guimarães
Aug 1, 1995·British Journal of Pharmacology·M O'RourkeJ R Docherty
Feb 1, 1997·General Pharmacology·J R Docherty, M O'Rourke

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Citations

Aug 31, 2001·European Journal of Pharmacology·C González-EspinosaJ A García-Sáinz
Mar 21, 2003·Vascular Pharmacology·Luz Elena Arévalo-LeónRafael Villalobos-Molina
Jul 31, 2007·European Journal of Pharmacology·Yoshitaka TomiyamaYoshinobu Yamazaki

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