WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties[2].In Vitro: WAY100135 (0.1-1 μM) antagonises electrically evoked contractions of 5-carboxamidoiodotryptamine in the guinea-pig ileum, with a pA2 of 7.2.
WAY-100135 dihydrochloride (10 μM) blocks the suppressive effect of 8-OH-DPAT on eEPSC and eIPSC in MVM neurons[2].In Vivo: WAY100135 (2.5 mg/kg) induces a maximum 30% inhibition of raphe neuronal firing and (0.5 mg/kg i.v.) antagonises the inhibition of firing induced by 8-OH-DPAT in anaesthetised rats.
WAY-100135 dihydrochloride (10 mM; 1 μL for microinjection) effectively abolishes all 5-HT induced behavioural deficits in rats[2].