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Cat. No. Product Name CAS No. Information
PC-62110

LY 2456302

1174130-61-0

LY 2456302 (CERC-501, JSPA 0658, Aticaprant) is a potent, selective, short-acting antagonist of κ-opioid receptor (KOR) with Ki of 0.81 nM; displays >30-fold selectivity over MOR and DOR; selectively and potently occupies central kappa opioid receptors in vivo (ED50=0.33 mg/kg); produces antidepressant-like effects in the mouse forced swim test and enhanced the effects of imipramine and citalopram; orally-bioavailable and excellent pharmacokinetic properties.

Depression

Phase 2 Clinical

PC-45162

Agomelatine L( )-Tartaric acid

824393-18-2

A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist; has no effect on monoamine uptake and no affinity for adrenergic, histaminergic, cholinergic, dopaminergic and benzodiazepine receptors, nor other serotonergic receptors; a melatonergic antidepressant treatment of major depressive disorder with relatively favorable side effect profile.

Depression

Approved

PC-35022

SR-57227 hydrochloride

77145-61-0 SR-57227 is a high affinity, selective 5-HT3 receptor agonist, demonstrates anticonvulsant effects in vivo.

Depression

Discontinued

PC-35021

SR-57227

77145-51-8 SR-57227 is a high affinity, selective 5-HT3 receptor agonist, demonstrates anticonvulsant effects in vivo.

Depression

Discontinued

PC-63400

JNJ-18038683

851376-05-1 JNJ-18038683 is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays; decreases 5-HT (100 nM)-stimulated adenylyl cyclase in rat and human 5-HT7/HEK293 cells with pKb of 8.01 and 7.99, respectively; shows 10-fold selectivity over h5-HT6 receptor, 15-fold selectivity over rat adrenergic α1 receptor, 14- to 25-fold selectivity over the h5-HT2 receptor subtypes, and 20-fold selectivity over h5-HT1B receptor; prolongs rapid eye movement (REM) sleep and decreases REM duration induced by citalopram in vivo.

Depression

Phase 2 Clinical

PC-63394

JNJ-39393406

953428-73-4 JNJ-39393406 is a potent, selective positive allosteric α7 nAChR modulator, potentiates a 100 μM choline-induced rise in intracellular calcium mediated by human α7 channels expressed in GH4C1 cells with EC50 of 660 nM; does not act on α4β2, α3β4 or 5-HT3A channels, as well as α4β2, α3β4 or 5 HT3A channels, and it does not interacts with a panel of 62 receptors and enzymes; shows bell-shaped dose-response activity in the auditory evoked potential (AEP) in DBA2 mice (0.63–5 mg/kg s.c., lower and higher doses were inactive), and model for sensory gating and the attentional set-shifting in rats.

Depression

Phase 2 Clinical

PC-63256

DSP-1053

1176326-78-5 DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively; inhibits serotonin transporter with IC50 of 2.74 nM and shows an intrinsic activity for 5-HT1A receptors of 70.0%; dose-dependently increases extracellular 5-HT levels in rat microdialysis at 3-10 mg/kg, demonstrates antidepressant-like effect in vivo.

Depression

Phase 1 Discontinued

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