Drug intelligence / Profile preview

CP-122,288

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

CP-122,288 is a potent and selective small molecule agonist of the serotonin receptor subtypes 5-HT1B, 5-HT1D, and 5-HT1F, developed as a derivative of sumatriptan for the treatment of migraine. While it dramatically surpasses sumatriptan in inhibiting neurogenic inflammation and plasma protein extravasation, it only marginally improves upon vascular constriction effects. Human clinical trials for migraine did not demonstrate efficacy, but its unique pharmacology has made it valuable for research into migraine pathophysiology and neurogenic inflammation[1][3][5][7].

Other names
N-Methyl-3-[1-methylpyrrolidin-2(R)-ylmethyl]-1H-indol-5-ylmethylsulfonamide5-(Methylaminosulfonylmethyl)-3-[1-methylpyrrolidin-2(R)-ylmethyl]-1H-indole
02

Targets

HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)HTR1F (Serotonin 5-HT1F receptor)

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