PNU-142633

PNU-142633 is an experimental, orally active small molecule that acts as a highly selective agonist of the serotonin 5-HT1D receptor. Developed by Pharmacia & Upjohn, it was investigated as an acute treatment for migraine attacks. Unlike traditional triptans, which target both 5-HT1B and 5-HT1D receptors, PNU-142633 was designed to selectively target 5-HT1D to avoid the vasoconstrictive cardiovascular side effects associated with 5-HT1B activation. However, in a Phase II clinical trial, a single 50 mg oral dose of PNU-142633 failed to demonstrate efficacy over placebo and was associated with adverse events such as chest pain and QTc prolongation. Consequently, its clinical development was discontinued, and it is currently utilized primarily as a research tool compound.

Other names

(1S)-1-{2-[4-(4-carbamoylphenyl)piperazin-1-yl]ethyl}-N-methyl-3,4-dihydro-1H-2-benzopyran-6-carboxamidePNU-142633 maleatePNU142633 maleatePNU 142633 maleate