| Identification | Back Directory | [Name]
5H-Pyrimido[4,5-d]azepin-4-amine, 2-(difluorophenylmethyl)-6,7,8,9-tetrahydro-N-methyl- | [CAS]
1065109-28-5 | [Synonyms]
PF-4522654
5H-Pyrimido[4,5-d]azepin-4-amine, 2-(difluorophenylmethyl)-6,7,8,9-tetrahydro-N-methyl- | [Molecular Formula]
C16H18F2N4 | [MOL File]
1065109-28-5.mol | [Molecular Weight]
304.34 |
| Hazard Information | Back Directory | [Uses]
PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI)[1]. | [IC 50]
5-HT2C Receptor: 16 nM (EC50); 5-HT2C Receptor: 8 nM (Ki); 5-HT2B Receptor: >10000 nM (EC50) | [References]
[1] R Ian Storer, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT?C) receptor agonists with exquisite functional selectivity over 5-HT?A and 5-HT?B receptors. J Med Chem. 2014 Jun 26;57(12):5258-69. DOI:10.1021/jm5003292 |
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