| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | PNU-142633 | ||||||||||||
| CAS | 187665-65-2 | ||||||||||||
| Formula | C24H30N4O3 | ||||||||||||
| Molar Mass | 422.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
PNU-142633
CAS: 187665-65-2 F: C24H30N4O3 W: 422.52
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for
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