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KMID : 0617319910010010014
Journal of Pharmacetical Sceiences Ewha Womans University
1991 Volume.1 No. 1 p.14 ~ p.25
LIGAND BINDING PROPERTIES OF ACETYLCHOLINE RECEPTOR FROM TORPEDO CALIFORNICA UNDER EQUIBRIUM CONDITIONS
Chang, Hai Won
Abstract
Studies of the bindings of agonists, such as [^3H]acetylcholine, [^3H]carbamoylcholine and [^14C]nicotine, to the acetylcholine receptor under conditions that should noramlly lead to a state of overall equilibrium did not give rese to a single equilibrium binding curves. Instead, the acetylcholine receptor was found to develop a metastable high affinity and lower affinity binding conformational states resulting in hysteresis in binding. It appears that the exposure of acetylcholine receptor to pulses of acetylcholine, as opposed to slow diffusion, stabilizes low-affinity, "desensitized" complexes. Our studies indicate that this hysteresis phenomenon in ligand binding is a general property of receptor agonists but, not of antagonists, and is likely to be related to receptor desensitization.
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