- Craig, D.A. et al. (1990) Naunyn Schmiedebergs Arch. Pharmacol. 342, 9.
- 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).
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.
2-Methyl-5-hydroxytryptamine hydrochloride (#M-170) is a highly pure, synthetic, and biologically active compound.