Size | Price | Stock |
---|---|---|
5mg | $400 | In-stock |
10mg | $680 | In-stock |
25mg | $1350 | In-stock |
50mg | $2200 | In-stock |
100mg | $3400 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-100330 |
M.Wt: | 243.30 |
Formula: | C14H17N3O |
Purity: | >98 % |
Solubility: | 10 mM in DMSO |
YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
IC50 & Target: Ki: 0.89±0.05 nM (5-HT2C receptor), 2.5±0.5 nM (5-HT2B receptor), 13±2 nM (5-HT2A receptor)[1]
EC50: 1.0±0.2 nM (5-HT2C receptor), 3.2±3 (5-HT2B receptor) , 93±10 nM (5-HT2A receptor)[1]
In Vitro: YM348 has high affinity for cloned human 5-HT2C receptors with a Ki value of 0.89 nM and lower affinities for human-cloned 5-HT2B (Ki: 2.5 nM) and 5-HT2A receptors (Ki: 13 nM). To assess the binding specificity of YM348, a broad evaluation of an additional 46 binding sites including several other 5-HT receptor subtypes (1A, 1B, 1D, 3, 4, 5A, 6, 7) is performed. IC50 values of YM348 are found to be >1 μM for all of the binding sites except for the human 5-HT1A receptors (Ki: 130 nM), bovine 5-HT1D receptors (Ki: 481 nM), human 5-HT7 receptors (Ki: 177 nM), and human α2A receptors (Ki: 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT2A and 5-HT2B receptors. The EC50 values of YM348 for 5-HT2C, 5-HT2A, and 5-HT2B receptors are 1.0, 93 and 3.2 nM, respectively[1].
In Vivo: Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT2C receptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg[1].
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