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Cat. No. Product Name CAS No. Information
PC-63187

RP-5063

1239729-06-6

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs; produces dose-dependent reductions in pulmonary blood vessel wall thickness and proportion of muscular vessels, blocks MCT-induced increases in the plasma cytokines TNFα, IL-1β, and IL-6 in vivo; prevents Sugen 5416-hypoxia-induced pulmonary arterial hypertension in rats; improves declarative memory and psychosis in mouse models of schizophrenia.

Schizophrenia

Phase 2 Clinical

PC-61105

MIN-101

359625-79-9

MIN-101 (Roluperidone, CYR-101, MT-210) is a higly potent 5-HT2A and sigma 2 receptor antagonist, with no direct dopamine affinities, for treatment of negative symptoms in schizophrenia.

Schizophrenia

Phase 3 Clinical

PC-60564

PF 05180999

1394033-54-5

PF-05180999 (PF 5180999) is a potent, selective, brain-penetrating and orally bioavailable phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 1 nM; displays >1,000-fold selectivity over PDE10; shows potential for treatment of schizophrenia.

Schizophrenia

Phase 1 Discontinued

PC-60496

AMG-579

1227067-61-9

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM; displays high selectivity with IC50 > 30 uM against all other PDE isoforms; demonstrates excellent target occupancy efficacy in PCP-LMA behavioral model.

Schizophrenia

Phase 1 Clinical

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-45900

LY-404039

635318-11-5

A potent, slective agonist of mGlu2 and mGlu3 receptors with Ki of 149 nM and 92 nM, respectively; displays >100-fold selectivity over other ionotropic glutamate receptors, glutamate transporters; suppresses electrically evoked excitatory activity in the striatum, and serotonin-induced l-glutamate release in the prefrontal cortex; reduces alcohol-seeking but not alcohol self-administration in alcohol-preferring (P) rats; oral bioavailable.

Schizophrenia

Phase 1 Clinical

PC-45821

PF-2545920

898562-94-2

A potent and selective PDE10A inhibitor with IC50 of 0.37 nM; displays >1,000-fold selectivity over the PDEs; antagonizes apomorphine-induced climbing in mice, inhibits conditioned avoidance responding in both rats and mice, and blocks NMDA antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats; dose-dependently increases c-Fos immunopositive nuclei in all regions of neostriatum in the DRd1a-tdTomato mice; improves cortico-basal ganglia function in huntington's disease models; orally bioavailable.

Schizophrenia

Phase 2 Discontinued

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