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PNU-142633

Catalog No. T16556 CAS 187665-65-2

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).

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PNU-142633, CAS 187665-65-2

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10 mg	4-5 weeks	$ 813.00

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Description	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).
Targets&IC50	5-HT1D receptor:6 nM （ki）
In vitro	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].
In vivo	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].

Molecular Weight	422.52
Formula	C24H30N4O3
CAS No.	187665-65-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

PNU-142633 187665-65-2 GPCR/G Protein Neuroscience 5-HT Receptor PNU142633 PNU 142633 inhibitor inhibit

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