The effect of the α1Q241L mutation on the activation and modulation
of concatemeric receptors. A, GABA dose-response properties for the
γβαQ241L-βα (hollow circles),
γβα-βαQ241L (hollow squares), and
γβαQ241L-βαQ241L receptors (filled diamonds). The
data show mean ± S.E.M. from 8-19 cells. The curves were fitted to the
Hill equation. The best-fit parameters are: EC50 = 140 ± 13
μM, nH = 1.4 ± 0.2
(γβαQ241L-βα); EC50 = 128 ± 8
μM, nH = 1.5 ± 0.1
(γβα-βαQ241L); EC50 = 152 ± 14
μM, nH = 1.5 ± 0.2
(γβαQ241L-βαQ241L). The dashed curve applies to
data from the wild-type γβα-βα receptor
(reproduced from Fig. 1B). B,
potentiation dose-response properties for the
γβαQ241L-βα (hollow circles),
γβα-βαQ241L (hollow squares), and
γβαQ241L-βαQ241L receptors (filled diamonds). The
data show mean ± S.E.M. from 4-6 cells. The test applications lasted 4
s and were separated from flanking control (30 μM GABA alone;
∼EC20) applications by 30 s washouts. The curve was fitted to
the Hill equation with an offset (fixed at 100%). The best-fit parameters for
the γβαQ241L-βα are: maximal potentiation = 313
± 27%, EC50 = 142 ± 65 nM. The best-fit parameters
for the γβα-βαQ241L are: maximal potentiation =
334 ± 28%, EC50 = 106 ± 41 nM. No fitting was
attempted for the data from the γβαQ241L-βαQ241L
receptor. The dashed curve applies to data from the wild-type
γβα-βα receptor (reproduced from
Fig. 5B).