Differential modulation by GTPγS of agnoist and inverse agonist binding to h5-HT_1A receptors revealed by[~3H]-WAY100,635

摘要

The interaction of erotonergic ligands at human(h)5-HT_1A receptors expressed in Chinese hamster ovary cells was examined with the selective 'neutral' 5-HT_1A antagonist[~3H]-WAY100,635. Its binding was saturable(K_D = 0.056 nM)with A B_max(3.65 pmol mg~-1)significantly higher than That of two other selective 5HT_1A radioligands; the partial agonist, [~3H]-S15535(2.77 pmol mg~-1) And the agonist,[~3H]-8-OH-DPAT(2.02 pmol mg~-1). The influence of GTPγS(100μM)on the binding affinity of 15 serotonergic agonists, partial Agonists, antagonists and inverse agonists was investigated in competition bindings experiments with [~3H]-WAY100,635.