| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
5-HT3 receptor (selective full agonist).
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|---|---|
| ln Vitro |
In vitro, 2-Methyl-5-HT acts as a selective 5-HT3 receptor agonist. It is used to study 5-HT3 receptor-mediated cellular responses, including ion channel activation, neurotransmitter release, and neuronal excitability. Quantitative in vitro activity data (e.g., EC50 for 5-HT3 receptor activation) is not detailed in publicly available sources.
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| ln Vivo |
2-Methyl-5-HT (2-methyl-5-hydroxytryptamine) exhibits antidepressant-like effects by significantly reducing immobility time [1].
In vivo, 2-Methyl-5-HT shows antidepressant-like effects in animal models. As a 5-HT3 receptor agonist, it modulates serotonergic signaling in the central nervous system. Detailed dose-response and pharmacokinetic data in vivo are limited in publicly available literature. |
| Enzyme Assay |
No specific cell-free receptor binding assay protocol is detailed for 2-Methyl-5-HT. For serotonin receptor agonists, typical cell-free assays include radioligand binding studies using [3H]GR65630 or [3H]BRL43694 for 5-HT3 receptors, or functional assays measuring calcium flux or electrophysiological responses in membrane preparations.
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| Cell Assay |
Cellular activity is assessed in heterologous cells expressing 5-HT3 receptors (e.g., HEK-293 cells). Cells are loaded with calcium-sensitive fluorescent dyes, treated with serial dilutions of 2-Methyl-5-HT, and calcium influx is measured using fluorometric imaging plate readers (FLIPR). EC50 values are calculated from concentration-response curves. Electrophysiology (patch-clamp) can also be used to measure 5-HT3 receptor-mediated currents.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats [1]
Doses: 3 mg/kg Route of Administration: intraperitoneal (ip) injection; 45 minutes Experimental Results: Dramatically diminished immobility time, thus showing an antidepressant-like effect. In vivo effects are evaluated in rodent models of depression or anxiety. 2-Methyl-5-HT is administered via intraperitoneal or intracerebroventricular injection. Behavioral tests (e.g., forced swim test, tail suspension test, elevated plus maze) are performed to assess antidepressant or anxiolytic-like effects. |
| ADME/Pharmacokinetics |
Molecular weight: 190.24; molecular formula: C11H14N2O. Purity: typically ≥98% for research use. Solubility: typical for tryptamine derivatives in DMSO or water. Storage: typical for small-molecule compounds (desiccated, protected from light, -20°C).
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a serotonin receptor agonist, potential toxicities may include serotonergic side effects (e.g., nausea, headache, cardiovascular effects). Standard toxicological studies would be required for drug development.
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| References | |
| Additional Infomation |
2-Methylserotonin belongs to the tryptamine class of compounds. It is a serotonergic agonist and is functionally related to serotonin.
2-Methyl-5-HT is a research-grade compound, not approved for therapeutic use. It is primarily used as a pharmacological tool for studying 5-HT3 receptor function and serotonergic signaling. No clinical trials have been reported. It is used in neuroscience research to investigate the role of 5-HT3 receptors in mood, cognition, and gastrointestinal function. |
| Molecular Formula |
C11H14N2O
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|---|---|
| Molecular Weight |
190.24166
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| Exact Mass |
190.111
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| CAS # |
78263-90-8
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| Related CAS # |
2-Methyl-5-HT hydrochloride;845861-49-6;2-Methyl-5-HT maleate;78263-91-9
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| PubChem CID |
1574
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| Appearance |
White to gray solid powder
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| Density |
1.242g/cm3
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| Boiling Point |
420.9ºC at 760 mmHg
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| Flash Point |
208.4ºC
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| Index of Refraction |
1.687
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| LogP |
2.383
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
198
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WYWNEDARFVJQSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H14N2O/c1-7-9(4-5-12)10-6-8(14)2-3-11(10)13-7/h2-3,6,13-14H,4-5,12H2,1H3
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| Chemical Name |
3-(2-aminoethyl)-2-methyl-1H-indol-5-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~657.06 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2565 mL | 26.2826 mL | 52.5652 mL | |
| 5 mM | 1.0513 mL | 5.2565 mL | 10.5130 mL | |
| 10 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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