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. 2010 Sep;334(3):761–774. doi: 10.1124/jpet.110.168211

TABLE 1.

Agonist and antagonist study on human nAChRs

Hα4β2 nAChRs
Hα3β4 nAChRs
EC50 or IC50 Valuea nH EC50 or IC50 Valuea nH
Epibatidine (EC50) 18.1 (6.5–50.6) nM 0.6 37.4 (10.7–71.4) nM 0.9
Nicotine (EC50) 8.9 (5.7–13.9) μM 1.2 9.1 (4.5–18.6) μM 0.9
d-tubocurarine (IC50) 2.3 (1.9–3.9) μM −0.7 1.6 (0.4–3.5) μM −0.9
Mecamylamine (IC50) 0.5 (0.3–0.8) μM −0.9 0.2 (0.1–0.3) μM −0.8
KAB-18 (IC50) 13.5 (9.7–18.5) μM −0.7 NA

nH, Hill coefficient; NA, no activity at concentrations up to 100 μM.

a

Values represent geometric means (confidence limits), n = 4–8.