Proceedings of the Korean Society of Embryo Transfer Conference (한국수정란이식학회:학술대회논문집)
- 2002.11a
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- Pages.96-96
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- 2002
SR144528 as Inverse Agonist of CB2 Cannabinoid Receptor
- M.H. Rhee (Dept. of Cell Biology & Physiology, Washington Univ., School of Medicine) ;
- Kim, S.K. (College of Vet., Med., Chungnam National University)
- Published : 2002.11.01
Abstract
We examined the role of SR 144528 (N-[-(1S-endo-1,3,,3-trimethyl-bicycle[2, 2, 1 ] heptan-2-y1]-5-(-4-chloro-3-mothyl-phenyl)-(4-methylbenzyl)-pyrazole-3- carboxamide) in the modulation of certain AC isoforms in transiently transfected COS-7 cells. We found that CB2 in COS cells has a constitutive activity, and thus leading to inhibition of AC-V activity even in the absence of agonist. In addition, this constitutive modulation of AC is reversed by SR144528. It is now well established that several G protein-coupled receptors can signal without agonist stimulation(constitutive receptors). Inverse agonists have been shown to inhibit the activity of such constitutive G protein-coupled receptor signaling. Agonist activation of the G
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