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. 2003 May 1;22(9):1990–2003. doi: 10.1093/emboj/cdg197

Table IV. Parameter values for the three-state allosteric kinetic mechanism for the α7/5HT3 receptor and mutants with five equivalent ACh binding sites per molecule.

α7/5HT3 receptor parameters
 
 
 
State parameters
B state
A state
D state
ACh on rates (M–1 s–1) Bkon = 107 Akon = 3.33 × 106 Dkon = 106
ACh off rates (s–1) Bkoff = 880 Akoff = 7.5 Dkoff = 1.6
Equilibrium constants (µM)
BKD = 88
AKD = 2.25
DKD = 1.6
Interconversion parameters
B↔A
A↔D
 
Transition state positional parameters BAp = 0.75 ADp = 0.99  
Interconversion rates (s–1) BAk5 = 22.8 ADk5 = 2.54  
  ABk5 = 0.107 DAk5 = 1.10  
  BAk0 = 0.233 ADk0 = 2.5  
  ABk0 = 105 DAk0 = 6.0  
Allosteric constants BAL0 = 4.3 × 105 ADL0 = 2.4  
 
BAL5 = 4.7 × 10–3
ADL5 = 0.43
 
G152Ka, P193I or G152K/P193I mutant parameters
 
 
 
State parameters
B state
A state
D state
ACh on rates (M–1 s–1) Bkon = 107 Akon = 3.33 × 106 Dkon = 106
ACh off rates (s–1) Bkoff = 1173.33 Akoff = 6.66 Dkoff = 1.42
Equilibrium constants (µM)
BKD = 117
AKD = 2.0
DKD = 1.42
Interconversion parameters
B↔A
A↔D
 
Transition state positional parameters BAp = 0.85 ADp = 0.99  
Interconversion rates (s–1) BAk5 = 63.5 ADk5 = 4.07  
  ABk5 = 3.06 × 10–6 DAk5 = 0.92  
  BAk0 = 3.0 ADk0 = 4.0  
  ABk0 = 100 DAk0 = 5.0  
Allosteric constants BAL0 = 33 ADL0 = 1.30  
  BAL5 = 4.82 × 10–8 ADL5 = 0.226  

aFor the G152K mutant, BKD = 33.2 µM, AKD = 1.2 µM and DKD = 0.2 µM.