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(S)-WAY 100135 dihydrochloride is a potent and selective antagonist of 5-HT1A receptor with IC50 value of 15 nM.

The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.

(S)-WAY 100135 dihydrochloride is a potent and selective somatodendritic and postsynaptic 5-HT1A receptors antagonist. (+/-)-WAY100135 inhibited 5-HT1A receptor in the rat hippocampal with IC50 value of 34 nM [1].

In the murine elevated plus-maze test, (S)-WAY 100135 (10 mg/kg) exhibited anxiolytic-like effects [2]. In free feeding rats, WAY-100135 (3 mg/kg) significantly inhibited hyperphagia and the increased incidence of feeding induced by 8-OH-DPAT (0.1 mg/kg), which was mediated by somatodendritic 5-HT1A autoreceptor [3]. In rats, (S)-WAY 100135 (0.2, 1, 5 ug/ul) inhibited the impairment of choice accuracy induced by intrahippocampal scopolamine (3.75 ug/ul) in a dose-dependent way. However, (S)-WAY 100135 didn’t influence the acquisition of spatial learning [4]. In rats, WAY-100135 (10.0 mg/kg) inhibited the decrease of 5-HT release induced by buspirone, a 5-HT1A receptor partial agonist [5].

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