S-8510 phosphate is an agonist of inverse Benzodiazepine (BDZ) receptor(Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively).

GABA+:36.2 nM (ki), GABA:ki： 34.6 nM

S-8510 exhibits high affinity for BDZ receptors with a GABA ratio similar to flumazenil, considered an antagonist or weak agonist. S-8510 (10-7 M) enhances LTP, an effect antagonized by the BDZ receptor antagonist flumazenil, which does not affect LTP on its own. S-8510 (10-4 M) increases the amplitude of the population spike, an effect fully antagonized by flumazenil (10-4 M).

S-8510 or CGS8216, in combination with PTZ doses exceeding 90 mg/kg, can induce lethal convulsions, specifically enhancing PTZ-induced subconvulsive states. Moreover, scopolamine impairs memory by reducing time spent near a platform, an effect both S-8510 and CGS8216 reverse, thereby mitigating scopolamine-induced amnesia. Additionally, S-8510 counters diazepam-induced memory impairments in both water maze and passive avoidance paradigms and elevates ACh levels up to 100 mg/kg in a dose-dependent manner. It, along with PTZ, also increases extracellular NA levels in the hippocampus. The anxiogenic effects of S-8510, CGS8216, and FG7142 were assessed in Wistar rats using the water lick conflict paradigm. In ddY mice, S-8510 significantly reduces immobility in the forced swimming test at doses ranging from 40 to 80 mg/kg, indicating a dose-dependent improvement in depressive symptoms. For tetrabenazine-induced ptosis, S-8510 effectively lessens ptosis at doses above 10 mg/kg, though at its maximum, it reduces ptosis by only 39%, in contrast to imipramine's more potent reduction of about 80% at 20 mg/kg.