Table 1.

Activation rate and equilibrium constants for wt AChRs

Agonists kon koff Kd Concentrations 
 mM−1s−1 s−1 M mM 
DMP 1,383 2,838 2.1 E-3 1, 2, 3 
DMT 1,991 3,194 1.6 E-3 1, 2, 3 
Nic 2,484 2,501 1 E-3 1, 2, 3 
TMA 6,770 5,515 0.81 E-3 0.3, 0.5, 0.7 
CCh 17,500 7,178 0.41 E-3 0.1, 0.2, 0.3, 0.5 
ACh 106,108 17,614 0.16 E-3 0.03, 0.1, 0.3 
Agonists kon koff Kd Concentrations 
 mM−1s−1 s−1 M mM 
DMP 1,383 2,838 2.1 E-3 1, 2, 3 
DMT 1,991 3,194 1.6 E-3 1, 2, 3 
Nic 2,484 2,501 1 E-3 1, 2, 3 
TMA 6,770 5,515 0.81 E-3 0.3, 0.5, 0.7 
CCh 17,500 7,178 0.41 E-3 0.1, 0.2, 0.3, 0.5 
ACh 106,108 17,614 0.16 E-3 0.03, 0.1, 0.3 

Concentrations are those used for the estimation of Kd. In all cases, the SEM of the rate constants were <10% of the optimal values shown. kon, koff, agonist association and dissociation rate constants to resting receptors; Kd (=koff/kon), the LA agonist equilibrium dissociation constant to resting receptors; Jd, the HA agonist equilibrium dissociation constant to open-channel (R*) receptors.

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