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PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research[1]. | [IC 50]
5-HT2C Receptor: 190 nM (EC50); 5-HT2C Receptor: 160 nM (Ki) | [References]
[1] Andrews MD, et al. Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorg Med Chem Lett. 2011 May 1;21(9):2715-20. DOI:10.1016/j.bmcl.2010.11.120 |
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