PNU-142633 has anti-migraine efficacy. PNU-142633 is a high affinity and selective 5-HT1D receptor agonist (Kis of 6 nM and >18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively).

Compared with 84% for that of Sumatriptan, in a cytosensor cell-based assay, the intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT [1].

PNU-142633 fails to alter resistance in these vascular beds. PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation [1].

187665-65-2

C24H30N4O3

422.52

PNU-142633

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years