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2-Methyl-5-hydroxytryptamine hydrochloride

Methyl serotonin

An Agonist of 5-HT3 and 5-HT6 Receptors

Cat #: M-170
Alternative Name Methyl serotonin
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 226.7
    Purity: >97%
    Effective concentration 0.5-50 µM.
    Chemical name 3-(2-aminoethyl)-2-methyl-1H-indol-5-ol;hydrochloride.
    Molecular formula C11H15ClN2O.
    CAS No.: 845861-49-6
    PubChem CID 11492320
    Activity Methyl serotonin is a 5-HT3 agonist (Ki = 1200 nM) and potent 5-HT6 ligand (Ki = 46 nM)1.
    1. Craig, D.A. et al. (1990) Naunyn Schmiedebergs Arch. Pharmacol. 342, 9.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs 2-Methyl-5-hydroxytryptamine hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.
      Alomone Labs 2-Methyl-5-hydroxytryptamine hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.
      Currents were elicited by 0.5 or 5 µM 2-Methyl-5-hydroxytryptamine hydrochloride (#M-170), as indicated. The currents elicited by this agonist were comparable in amplitude to the cells responses to 10 µM 5-HT (not shown here).
    References - Scientific background
    1. Hannon, J. and Hoyer, D. (2008) Behav. Brain Res. 195, 198.
    2. Edwards, E.  et al. (1991) Brain Res. 545, 276.
    3. Sepulveda, M.I. et al. (1991) Br. J. Pharmacol. 104, 536.
    Scientific background

    Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.

    Methyl Serotonin (2-Methyl-5-hydroxytryptamine hydrochloride) is an agonist of 5-HT3 receptors with an effective concentration of 0.5-50 µM and an IC50 of 3.1±0.9 µM and also a potent ligand of the 5-HT6 receptor, member of the G-protein coupled receptor superfamily. Methyl Serotonin mimics the action of 5-HT although it displays a low affinity to 5-HT1 and 5-HT2 receptors. Methyl Serotonin was found to stimulate the hydrolysis of phosphoinositide in rat brain tissue2. In a study conducted in N1E-115 neuroblastoma cells, Methyl Serotonin elicited inward ion currents that were only 19.9±2.4% of currents elicited by regular Serotonin binding. These currents increase with higher concentration of Methyl serotonin. Desensitization of the 5-HT receptor after Methyl Serotonin binding was slower than equivalent Serotonin binding3.

    Target 5-HT3 and 5-HT6 receptors
    Last update: 06/11/2022

    2-Methyl-5-hydroxytryptamine hydrochloride (#M-170) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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