| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Salsolidine targets monoamine oxidase A (MAO A), an enzyme responsible for the oxidative deamination of monoamine neurotransmitters including serotonin, norepinephrine, and dopamine. It acts as a stereoselective competitive inhibitor of MAO A. The compound also inhibits catechol-O-methyltransferase (COMT) with a Ki of 190 uM. By inhibiting these enzymes, salsolidine affects neurotransmitter metabolism.
|
|---|---|
| ln Vitro |
Tetrahydroisoquinoline alkaloid salsolidine functions as a competitive, stereoselective MAO A inhibitor. Compared to S-salsolidine, R-salsolidine exhibits greater activity against MAO A (Ki of 186 μM against 6 μM) [1]. Salsolidine has a Ki >100 μM and mildly inhibits δ-receptor binding [2]. Acetylcholinesterase and butyrylcholinesterase may be inhibited by salsolidine [3].
In vitro, salsolidine acts as a stereoselective competitive MAO A inhibitor. It also inhibits catechol-O-methyltransferase (COMT) with a Ki of 190 uM. The compound's activity as a MAO A inhibitor has been characterized in enzyme assays measuring the oxidative deamination of monoamine substrates. Its stereoselectivity suggests that the compound's inhibitory activity depends on its stereochemical configuration. |
| ln Vivo |
In vivo activity of salsolidine is inferred from its mechanism as a MAO A and COMT inhibitor. As a tetrahydroisoquinoline alkaloid, it may have effects on neurotransmitter levels and related physiological processes. However, detailed in vivo data for salsolidine are limited in the available literature. The compound is a naturally occurring alkaloid and is used primarily as a research tool for studying MAO A and COMT inhibition.
|
| Enzyme Assay |
The in vitro enzyme assay for salsolidine involves measuring MAO A inhibition. MAO A enzyme (typically from human recombinant sources or rat liver mitochondria) is incubated with varying concentrations of salsolidine (typically 0.001-1000 uM) and a substrate such as serotonin, kynuramine, or tyramine in appropriate buffer (e.g., 0.1 M phosphate buffer, pH 7.4) at 37degC for 30-60 minutes. The reaction is stopped by the addition of an acid or base, and the product is measured spectrophotometrically or fluorometrically. For COMT inhibition, the compound is incubated with COMT and a substrate such as catechol or dopamine, and the methylated product is measured by HPLC or radiometric methods.
|
| Cell Assay |
In vitro cellular assays for salsolidine are conducted using neuronal cell lines or cell lines expressing MAO A. Cells are seeded in multi-well plates and treated with varying concentrations of salsolidine (typically 0.01-1000 uM) for 24-72 hours. MAO A activity in cell lysates is measured using fluorometric or colorimetric assays with MAO substrates. Neurotransmitter levels (serotonin, norepinephrine, dopamine) in cell culture supernatants or cell lysates are measured by HPLC or ELISA. Cell viability is monitored using MTT or similar assays to ensure that observed effects are not due to cytotoxicity.
|
| Animal Protocol |
In vivo animal studies for salsolidine are not extensively documented. As a research compound with MAO A and COMT inhibitory activity, typical studies would involve administration to rodents to assess its effects on neurotransmitter levels, behavior, and physiological parameters. The compound would be administered by intraperitoneal injection or oral gavage at doses determined from preliminary pharmacokinetic and tolerability studies. Brain neurotransmitter levels would be measured by HPLC, and behavioral tests such as open field or forced swim tests might be performed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of salsolidine are not extensively documented. The compound has a molecular weight of 207.27 and a molecular formula of C12H17NO2. It is soluble in DMSO at 50 mg/mL (241.23 mM). As a small, lipophilic alkaloid, it is expected to have good oral bioavailability and the ability to cross the blood-brain barrier. The compound should be stored under appropriate conditions as recommended by the supplier. Detailed ADME parameters are not available in the published literature.
|
| Toxicity/Toxicokinetics |
The toxicological profile of salsolidine has not been extensively characterized. As a MAO A inhibitor, the compound may have effects on neurotransmitter levels and potential toxicity at high doses. MAO inhibitors can cause side effects related to increased monoamine levels, including hypertension and serotonin syndrome when combined with serotonergic drugs. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling the compound.
|
| References |
|
| Additional Infomation |
6,7-Dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinoline belongs to the isoquinoline class of compounds. It has been reported to be detected in Haloxylon salicornicum, Carnegiea gigantea, and Calobota pungens, with relevant data available. See also: Salt-based sulfadiazine (note moved to).
Salsolidine (CAS 5784-74-7) is a tetrahydroisoquinoline alkaloid that acts as a stereoselective competitive MAO A inhibitor. It also inhibits catechol-O-methyltransferase (COMT) with a Ki of 190 uM. The compound has been found in H. articulatum and is used as a research tool for studying neurotransmitter metabolism. It is available for research purposes only. |
| Molecular Formula |
C12H17NO2
|
|---|---|
| Molecular Weight |
207.268883466721
|
| Exact Mass |
207.126
|
| CAS # |
5784-74-7
|
| Related CAS # |
Salsolidine hydrochloride;63283-42-1;(S)-Salsolidine;493-48-1
|
| PubChem CID |
10302
|
| Appearance |
Light yellow to brown solid powder
|
| Density |
1.034g/cm3
|
| Boiling Point |
313.4ºC at 760 mmHg
|
| Flash Point |
127.1ºC
|
| LogP |
2.239
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
15
|
| Complexity |
210
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
HMYJLVDKPJHJCF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H17NO2/c1-8-10-7-12(15-3)11(14-2)6-9(10)4-5-13-8/h6-8,13H,4-5H2,1-3H3
|
| Chemical Name |
6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinoline
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~241.23 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.06 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 25.0 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: ≥ 2.5 mg/mL (12.06 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 25.0 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 | 4.8246 mL | 24.1231 mL | 48.2462 mL | |
| 5 mM | 0.9649 mL | 4.8246 mL | 9.6492 mL | |
| 10 mM | 0.4825 mL | 2.4123 mL | 4.8246 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
