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PNU-22394 hydrochloride is an agonist for 5-HT, with Ki of 6.1 and 10 nM, for 5-HT2C and 5-HT2A, respectively[1]. | [in vivo]
PNU-22394 hydrochloride exhibits agonistic efficacy for 5-HT2C and 5-HT2A, with EC50 of 7.7 and 23 nM (measured via the Fluo-4/Ca2+ Assay), or 0.12 and 0.21 μM (measured via IP-One Assay), while the Rmax is 97%-102%[2]. | [References]
[1] Ennis MD, et al., 2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2369-72. DOI:10.1016/s0960-894x(03)00403-7
[2] Jensen AA, et al., Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. J Med Chem. 2013 Feb 14;56(3):1211-27. DOI:10.1021/jm301656h |
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