TABLE 2

Selectivity of PAMs at other human nAChR subtypes studied by Ca2+ imaging




HEK α4β2 pEC50 [Max-fold]a

HEK α3β4 pEC50 [Max-fold]a
PNU-120596 N.A. [0.89 ± 0.11]b (n = 4) N.A. [0.80 ± 0.08]b (n = 4)
TQS 5.3 ± 0.2 [0.27 ± 0.04] (n = 4) N.A. [0.89 ± 0.07]c (n = 4)
5-HI 3.4 ± 0.1 [0.21 ± 2.7] (n = 6) 2.9 ± 0.2 [0.28 ± 2.7] (n = 4)
Genistein
N.A. [0.60 ± 0.07]d (n = 6)
N.A. [0.63 ± 0.10]d (n = 4)
  • a Normalized to 3 to 10 μM nicotine.

  • b Effect at 30 μM.

  • c Effect at 10 μM.

  • d Effect at 100 μM.