Mar. 7th, 2006
(no subject)
Mar. 7th, 2006 08:13 pmFigure 3. When we examine a transfected system, basal activity is a measurable amount since there is a 1000 fold higher number of receptors compared to the native system. This means that there are 1000 times as many receptors that randomly assume the active conformation vs. native cells. Thus, constitutive receptor activity is measurable in the absence of agonist. In this case, addition of agonist alone also produces a classical concentration-response. Addition of antagonist alone will produce no response. Addition of the inverse agonist stabilizes the inactive conformation of the receptor and drives the equilibrium away from the active conformation. Thus addition of inverse agonist reduces the constitutive activity of the receptor and inhibits basal activity.
KEEN
1. http://medicine.creighton.edu/pharmacology/inverse.htm