1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. YM348


Cat. No.: HY-100330
Handling Instructions

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).

For research use only. We do not sell to patients.

YM348 Chemical Structure

YM348 Chemical Structure

CAS No. : 372163-84-3

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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[1]

5-HT2C Receptor

0.89 nM (Ki)

5-HT2B Receptor

2.5 nM (Ki)

5-HT2A Receptor

13 nM (Ki)

5-HT2C Receptor

1 nM (EC50)

5-HT2B Receptor

3.2 nM (EC50)

5-HT2A Receptor

93 nM (EC50)

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].

Molecular Weight







C[[email protected]](N)CN(N=C1)C2=C1C=CC3=C2C=C(CC)O3


Room temperature in continental US; may vary elsewhere


Please store the product under the recommended conditions in the Certificate of Analysis.

Kinase Assay

Experiments are performed with membranes obtained from Chinese Hamster Ovary (CHO) cells expressing human 5-HT2C or 5-HT2A receptors and Human Embryonic Kidney 293-Epstein-Barr virus nuclear antigen (HEK293-EBNA) cells expressing human 5-HT2B receptors. Binding assays with [3H] 5-HT are carried out. The reaction medium (50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl2, 10 M pargyline and 0.1 mg/ml L-(+)-ascorbic acid) containing [3H] 5-HT, membrane preparation and test compounds are incubated at 37°C for 30 min. Nonspecific binding is determined in the presence of 10 M 5-HT, and specific binding is calculated as the total binding minus the nonspecific binding. After incubation, 4 mL of 50 mM Tris-HCl buffer (pH 7.4) containing 4 mM CaCl2 is added, and the medium is filtrated under decompression through a Whatman GF/B glass filter pretreated with 0.1% polyethyleneimine. The filter is washed with the same buffer solution (4 mL×3). The glass filter is immersed in 6 mL of liquid scintillator (Packard, Aquasol-2), and the radioactivity is measured with a liquid scintillation counter. The amount of protein is measured. The dissociation constants (Kd values) are obtained by Scatchard analysis using SAS (ver. 6.11). The concentrations of compounds showing 50% inhibition of receptor binding, IC50 values, are obtained by nonlinear analysis using SAS (ver. 6.11). The Ki values indicating affinity for receptors are calculated[1].

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

Animal Administration

Male Wistar rats (215-350 g) are used. Rats are administered YM348 (0.0677, 0.203, 0.677, and 2.03 mg/kg) orally and moved again to their home cages. After 20 min, thereafter, the rats are individually placed in transparent acrylic plastic cages (35×30×18 cm), and their motor activity is measured for 40 min. The measurements are carried out using a SUPER-MEX sensor. SB242084 (0.1-3 mg/kg i.p.) is administered 30 min before YM348 treatment.

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

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