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Cat. No. Product Name CAS No. Information
PC-61625

Befiradol

208110-64-9

Befiradol (F13640, NLX 112) is a highly potent, selective 5-HT1A receptor agonist with Ki of 2.7 nM; exhibits agonist efficacy greater than for (±)8-OH-DPAT or buspirone; stimulates 'total G-proteins', but unlike (±)8-OH-DPAT and buspirone, more potent for Gαo activation, in rat hippocampal membranes; dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC in rats, activates both 5-HT(1A) autoreceptors and postsynaptic 5-HT(1A) receptors in prefrontal cortex with a similar potency.

Pain

Discontinued

PC-61522

SUVN-502 mesylate hydrate

1791396-45-6

SUVN-502 (SUVN502) is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with Ki of 2.04 nM; shows high selectivity over 5-HT2A receptor and other 100 target sites; produces synergistic effects in extracellular levels of acetylcholine in the ventral hippocampus combined with donepezil and memantine; shows potential for treatment of Alzheimer's disease.

Alzheimer Disease

Phase 2 Clinical

PC-61521

SUVN-502 mesylate

1791396-46-7

SUVN-502 (SUVN502) is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with Ki of 2.04 nM; shows high selectivity over 5-HT2A receptor and other 100 target sites; produces synergistic effects in extracellular levels of acetylcholine in the ventral hippocampus combined with donepezil and memantine; shows potential for treatment of Alzheimer's disease.

Alzheimer Disease

Phase 2 Clinical

PC-61500

SUVN-502

701205-60-9

SUVN-502 (SUVN502, Masupirdine) is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with Ki of 2.04 nM; shows high selectivity over 5-HT2A receptor and other 100 target sites; produces synergistic effects in extracellular levels of acetylcholine in the ventral hippocampus combined with donepezil and memantine; shows potential for treatment of Alzheimer's disease.

Alzheimer Disease

Phase 2 Clinical

PC-60521

Minesapride

1184662-54-1

Minesapride (DSP-6952) is a novel potent, selective, orally active 5-HT4 receptor partial agonist with Ki of 50-100 nM for human 5-HT4a/4b/4c; enhances gastric motility and causes colonic giant migrating contractions (GMCs) associated with defecation in conscious dogs, having ED50 value for inducing GMCs of 1.56 mg/kg; rapidly increases fecal wet weight without increasing fluid content in mice (1-10 mg/kg, p.o.).

PC-70076

Lumateperone

313368-91-1

Lumateperone (ITI-007) is a potent 5-HT2A antagonist (Ki=0.54 nM), postsynaptic D2 antagonist(Ki=32 nM), and SERT blocker (Ki= 61 nM); also shows affinity for D1; orally bioavailable and exhibits good antipsychotic efficacy in vivo.

Schizophrenia

Phase 3 Clinical

PC-35384

EMD-281014 hydrochloride

443144-27-2 EMD-281014 hydrochloride ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.

Sleep Disorder

Discontinued

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