TABLE 3

Affinities (pKA) of the allosteric agents to bind to the indicated wild-type and mutant receptors and factors of cooperativity (pα) for the interaction with [3H]NMS equilibrium binding

pKA is the -log equilibrium dissociation constant for allosteric agent binding to NMS-free receptors. pα is the -log value of the cooperativity factor; a positive or negative pα reflects an elevation or reduction of [3H]NMS equilibrium binding, respectively. Data are presented as means ± S.E. of three to four separate experiments with duplicated values.

M2 M2-Y177→Q + T423→H M5
Diallylcaracurine V
    pKA 7.76±0.06a 6.93±0.09 5.95±0.06
    pα 0.24±0.06 -1.47±0.003 -0.99±0.06
W84
    pKA 8.15±0.12 6.84±0.06 N.D.
    pα -0.81±0.08 -1.01±0.13 N.D.
Dimethyl-W84
    pKA 9.02±0.01 7.57±0.05 N.D.
    pα -1.04±0.04 -1.61±0.08 N.D.
  • N.D., not determined

  • a EC0.5,diss was used for curve fitting as described under Materials and Methods