TABLE 1

Agonist and antagonist study on human nAChRs

Hα4β2 nAChRsHα3β4 nAChRs
EC50 or IC50 ValueanHEC50 or IC50 ValueanH
Epibatidine (EC50)18.1 (6.5–50.6) nM0.637.4 (10.7–71.4) nM0.9
Nicotine (EC50)8.9 (5.7–13.9) μM1.29.1 (4.5–18.6) μM0.9
d-tubocurarine (IC50)2.3 (1.9–3.9) μM−0.71.6 (0.4–3.5) μM−0.9
Mecamylamine (IC50)0.5 (0.3–0.8) μM−0.90.2 (0.1–0.3) μM−0.8
KAB-18 (IC50)13.5 (9.7–18.5) μM−0.7NA
  • nH, Hill coefficient; NA, no activity at concentrations up to 100 μM.

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