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CP-809101

Development stage: Discontinued
Lead developer: Pfizer
Modality: Small Molecules
Administration: Subcutaneous, Intraperitoneal

Overview

CP-809101 is a potent and highly selective 5-HT2C receptor agonist (pEC50 = 9.96 for human 5-HT2C) developed by **Pfizer**. It displays approximately 100% efficacy in vitro and demonstrated antipsychotic-like activity in preclinical models, including suppression of conditioned avoidance responding and inhibition of PCP and amphetamine-stimulated hyperactivity. The compound showed low extrapyramidal symptom liability and activity in cognitive function models. However, it was associated with genotoxicity, restricting future use to research applications only.

Other names: 2-[(3-Chlorophenyl)methoxy]-6-(1-piperazinyl)pyrazine2-((3-chlorobenzyl)oxy)-6-(piperazin-1-yl)pyrazine

Targets

HTR2C (5-hydroxytryptamine 2C receptor)HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)

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