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J. Biol. Chem., Vol. 269, Issue 42, 25970-25973, 10, 1994
LM Leeb-Lundberg, SA Mathis and MC Herzig
Several B2 bradykinin (BK) receptor-specific antagonists including HOE140,
NPC17731, and NPC567 exhibited negative intrinsic activity, which was
observed as a decrease in basal phosphoinositide hydrolysis in primary
cultures of rat myometrial cells, and this response was opposite to that
elicited by the agonist BK. The order of potency of the antagonists in
attenuating basal activity was essentially the same as that in competing
both [3H]BK and [3H]NPC17731 for binding to B2 receptors on both intact rat
myometrial cells and bovine myometrial membranes. We previously proposed a
three-state model for the binding of agonists to G-protein-coupled B2
receptors in bovine myometrial membranes (Leeb-Lundberg, L. M. F. and
Mathis, S. A. (1990) J. Biol. Chem. 265, 9621-9627). This model was based
on the ability of BK to promote the sequential formation of three receptor
binding states where formation of the third, equilibrium state was blocked
by Gpp(NH)p (guanyl-5'-yl imidodiphosphate) identifying it as the
G-protein-coupled state of the receptor. Here, we show that, in contrast to
BK, these antagonists bound preferentially to a G-protein-uncoupled state
of the receptor. These results indicate that B2 receptor antagonists that
stabilize a G-protein-uncoupled state of the receptor act as inverse
agonists. Furthermore, these results provide strong evidence that
endogenous G-protein-coupled receptors exhibit spontaneous activity in
their natural environment in the absence of agonist occupancy.
Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells
Department of Biochemistry, University of Texas Health Science Center, San Antonio 78284-7760.
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