YM348 

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

YM348 has high affinity for cloned human 5-HT_2C receptors with a K_i value of 0.89 nM and lower affinities for human-cloned 5-HT_2B (K_i: 2.5 nM) and 5-HT_2A receptors (K_i: 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-HT_1A receptors (K_i: 130 nM), bovine 5-HT_1D receptors (K_i: 481 nM), human 5-HT₇ receptors (K_i: 177 nM), and human α_2A receptors (K_i: 126 nM).YM348 exhibits a full-agonistic activity on human 5-HT_2A and 5-HT_2B receptors. The EC₅₀ values of YM348 for 5-HT_2C, 5-HT_2A, and 5-HT_2B receptors are 1.0, 93 and 3.2 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Oral administration of YM348 induces penile erections and hypolocomotion in rats, being completely inhibited by a selective 5-HT_2C receptor antagonist, SB242084. YM348 inhibits spontaneous activity in a dose-dependent manner with a minimum effective dose of 0.203 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

243.30

C₁₄H₁₇N₃O

372163-84-3

Oil

Light yellow to brown

C[C@H](N)CN(N=C1)C2=C1C=CC3=C2C=C(CC)O3

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Kimura Y, et al. Pharmacological profile of YM348, a novel, potent and orally active 5-HT_2C receptor agonist. Eur J Pharmacol. 2004 Jan 1;483(1):37-43.  [Content Brief]