Table 2. Comparison of potency and efficacy of nAChR agonists on recombinant human nAChRs expressed on Xenopus Oocytes

Agonist

ha2b2

ha2b4

ha3b2

ha3b4

ha4b2

ha4b4

ha7

ACh

 

 

 

 

 

 

 

EC50

68.67 mM

82.57 mM

442.90 mM

203.14 mM

68.05 mM

19.68 mM

179.57 mM

Imax

1.25

1.25

5.0

1.25

1.25

1.25

1.25

 

 

 

 

 

 

 

 

NIC

 

 

 

 

 

 

 

EC50

19.23 mM

20.71 mM

132.44 mM

80.30 mM

5.47 mM

5.02 mM

113.34 mM

Imax

0.77 0.11

1.03 0.07

2.84 0.52

0.78 0.05

0.52 0.12

1.0 0.05

1.38 0.11

 

 

 

 

 

 

 

 

DMPP

 

 

 

 

 

 

 

EC50

11.18 mM

22.77 mM

55.87 mM

18.67 mM

17.99 mM

18.71 mM

30.86 mM

Imax

0.53 0.02

0.36 0.02

11.20 1.42

0.98 0.07

0.14 0.05

0.42 0.05

1.02 0.01

 

 

 

 

 

 

 

 

CYT

 

 

 

 

 

 

 

EC50

25.43 mM

38.86 mM

67.09 mM

72.18 mM

2.61 mM

0.90 mM

71.42 mM

Imax

0.13 0.02

0.29 0.08

0.038 0.003

0.60 0.04

0.06 0.01

0.51 0.06

1.16 0.03

a Potency (EC50) expressed as geometric mean, and efficacy (Imax) are expressed as the arithmetic mean S.E.M.

Imax represents the fraction of the ACh ED80 response (EC20 for ha3b2). N = 4-6. Data taken from Chavez-Noriega et al., 1997.

 

published 2000