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. 2012 Jul;140(1):17–28. doi: 10.1085/jgp.201210801

Figure 1.

Figure 1.

Activation of AChRs by CCh. (A) Low resolution view of current clusters that reflect binding and gating activity of single AChRs (+70 mV; open is up). (B) Higher resolution view of clusters at different [CCh] and corresponding intra-cluster interval duration histograms. Solid lines are the global fit by boxed states in D. (C) With increasing [CCh], the effective opening rate reaches a plateau that is the diliganded opening rate constant. (D) Cyclic model for binding and gating. R, LA/closed-channel conformation; R*, HA/open-channel conformation; A, agonist; Kd, equilibrium dissociation constant of R; Jd, equilibrium dissociation constant of R*. E0, E1, and E2 are gating equilibrium constants with zero, one, and two bound agonists. When the two binding sites are functionally equivalent, E2/E0 = (Kd/Jd)2 and E1/E0 = E2/E1. The rate constants: kon, LA association; koff, LA dissociation; f2, diliganded opening; b2, diliganded closing. (E) Agonist structures.