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PNU 142633

Names

[ CAS No. ]:
187665-65-2

[ Name ]:
PNU 142633

[Synonym ]:
unii-b54p1bq73l

Biological Activity

[Description]:

PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1D Receptor:6 nM (Ki)


[In Vitro]

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

[In Vivo]

PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds[1]. Animal Model: Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode[1] Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg Administration: Intravenous injection Result: Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.

[References]

[1]. McCall RB, et al. Preclinical studies characterizing the anti-migraine and cardiovascular effects of the selective 5-HT1D receptor agonist PNU-142633. Cephalalgia. 2002 Dec;22(10):799-806.

[2]. Gomez-Mancilla B, et al. Safety and efficacy of PNU-142633, a selective 5-HT1D agonist, in patients with acute migraine. Cephalalgia. 2001 Sep;21(7):727-32.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H30N4O3

[ Molecular Weight ]:
422.52000

[ Exact Mass ]:
422.23200

[ PSA ]:
87.90000

[ LogP ]:
3.06530

[ Storage condition ]:
2-8°C

Related Compounds