| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
5-HT1 Receptor 5-HT2 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor Human Endogenous Metabolite
5-Methoxytryptamine hydrochloride targets multiple serotonin (5-HT) receptor subtypes. It acts as a non-selective full agonist at 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors, while having no affinity for the 5-HT3 receptor. It shows binding affinity for the rat brain 5-HT1A receptor with a Ki of 11 nM. By activating these receptors, the compound modulates serotonergic signaling pathways involved in mood regulation, gastrointestinal motility, and neurotransmitter release. |
|---|---|
| ln Vitro |
In vitro, 5-Methoxytryptamine hydrochloride acts as a non-selective full agonist at multiple 5-HT receptor subtypes. Its activity is typically assessed by measuring its ability to stimulate cAMP accumulation or calcium mobilization in cells expressing various 5-HT receptors. The compound exhibits antioxidant properties in cell-based assays. It is used as a research reagent for serotonin receptor assays and to study the role of serotonergic signaling in various physiological and pathological processes.
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| ln Vivo |
5-Methoxytryptamine hydrochloride causes rats to have severe hyperglycemia when given more than 1 mg/kg[1].
In vivo, 5-Methoxytryptamine hydrochloride is used in research to study serotonin receptor-mediated effects. As a metabolite of Melatonin, it may contribute to the physiological effects of melatonin through serotonin receptor activation. The compound's non-selective agonist profile makes it useful for studying the integrated effects of serotonin receptor activation. Its radioprotective properties have been investigated in pre-clinical models. However, comprehensive in vivo pharmacological studies are limited. |
| Enzyme Assay |
For non-cell-based receptor binding assays, 5-Methoxytryptamine hydrochloride can be evaluated using membrane preparations from tissues or cells expressing various 5-HT receptor subtypes. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-8-OH-DPAT for 5-HT1A, [3H]-ketanserin for 5-HT2A, or [3H]-GR113808 for 5-HT4. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing various 5-HT receptor subtypes are cultured in appropriate media. For functional assays, the appropriate signaling readout is measured depending on the receptor subtype (e.g., cAMP accumulation for Gs-coupled receptors, calcium mobilization for Gq-coupled receptors). Cells are treated with various concentrations of 5-Methoxytryptamine hydrochloride, and the signaling response is measured using fluorescent indicators or ELISA-based detection. EC50 values are calculated from dose-response curves. For antioxidant assays, cells are treated with oxidative stressors in the presence or absence of the compound, and oxidative stress markers are measured.
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| Animal Protocol |
For in vivo animal studies, 5-Methoxytryptamine hydrochloride can be administered to rodents via intraperitoneal injection. In models of serotonin-mediated behaviors, its effects on locomotion, anxiety, and gastrointestinal motility are assessed. In radioprotection studies, the compound's ability to protect against radiation-induced damage is evaluated. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
5-Methoxytryptamine hydrochloride has a molecular weight of 226.70 and a molecular formula of C11H15ClN2O. It is supplied as a crystalline solid with a purity of ≥98%. The compound is soluble in water and DMSO. It should be stored at -20°C for long-term stability. It is provided as a research-grade reagent for studies of serotonin receptor activity, antioxidant effects, and radioprotective actions in biochemical and neuroscience applications.
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| Toxicity/Toxicokinetics |
The toxicity profile of 5-Methoxytryptamine hydrochloride has not been extensively reported. As a non-selective serotonin receptor agonist, potential adverse effects may include modulation of serotonergic signaling, which could affect mood, gastrointestinal function, and cardiovascular regulation. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound.
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| References |
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| Additional Infomation |
See also: 5-methoxytryptamine (note moved to).
5-Methoxytryptamine hydrochloride (CAS 66-83-1) is a non-selective serotonin receptor agonist that acts as a full agonist at multiple 5-HT receptor subtypes including 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7, while exhibiting negligible affinity for the 5-HT3 receptor. It is a metabolite of Melatonin and exhibits antioxidant and radioprotective properties. It is used in biochemical and neuroscience applications to study serotonin receptor activity. It is available for research purposes only. |
| Molecular Formula |
C11H15CLN2O
|
|---|---|
| Molecular Weight |
226.70
|
| Exact Mass |
226.087
|
| CAS # |
66-83-1
|
| Related CAS # |
5-Methoxytryptamine;608-07-1
|
| PubChem CID |
6198
|
| Appearance |
White to off-white solid powder
|
| Density |
1.171 g/cm3
|
| Boiling Point |
380ºC at 760 mmHg
|
| Melting Point |
246 °C
|
| Flash Point |
183.6ºC
|
| LogP |
3.18
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
15
|
| Complexity |
186
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC2=C(C=C1)NC=C2CCN.Cl
|
| InChi Key |
TXVAYRSEKRMEIF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H14N2O.ClH/c1-14-9-2-3-11-10(6-9)8(4-5-12)7-13-11;/h2-3,6-7,13H,4-5,12H2,1H3;1H
|
| Chemical Name |
2-(5-methoxy-1H-indol-3-yl)ethanamine;hydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4111 mL | 22.0556 mL | 44.1112 mL | |
| 5 mM | 0.8822 mL | 4.4111 mL | 8.8222 mL | |
| 10 mM | 0.4411 mL | 2.2056 mL | 4.4111 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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