Table 1

Expression of [3H]ketanserin binding by native and mutant 5-HT2A receptors

Drug5-HT2AW76AF125LW200AW336AF339LF340LF365LW367AY370AF383A
Kd (nm)0.98  ± 0.39.8  ± 0.71.5  ± 1.30.65  (n = 2)899  ± 1338  ± 3.82.2  ± 0.83.9  ± 1.4N.D.18.4  (n = 2)3.5  (n = 2)
Bmax (fmol/mg of protein)1900  ± 2501763  ± 1522150  ± 248400  (n = 2)296  ± 130912  ± 1501100  ± 1371862  ± 428N.D.1382  ± 4142820  ± 225

Data represent mean ± standard deviation of computer-derived estimates for three separate experiments, except where noted. For the W336A, F339L, and Y370A mutants, [3H]mesulergine was used as the radioligand. For all other mutants, [3H]ketanserin was used. In a typical experiment, 90% of total binding was specific, and ≤10% of the total radioligand was bound.B max data for the F125L, F339L, and F340L mutations are from Ref. 3.

    • N.D., no binding detected.