187665-65-2
187665-65-2 structure
- Name: PNU 142633
- Chemical Name: (1S)-1-[2-[4-(4-carbamoylphenyl)piperazin-1-yl]ethyl]-N-methyl-3,4-dihydro-1H-isochromene-6-carboxamide
- CAS Number: 187665-65-2
- Molecular Formula: C24H30N4O3
- Molecular Weight: 422.52000
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2016-07-19 04:43:56
- Modify Date: 2024-01-08 19:23:56
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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].
| Name | (1S)-1-[2-[4-(4-carbamoylphenyl)piperazin-1-yl]ethyl]-N-methyl-3,4-dihydro-1H-isochromene-6-carboxamide |
|---|---|
| Synonyms | unii-b54p1bq73l |
| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C24H30N4O3 |
|---|---|
| Molecular Weight | 422.52000 |
| Exact Mass | 422.23200 |
| PSA | 87.90000 |
| LogP | 3.06530 |
| Storage condition | 2-8°C |