| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
The benzodiazepine binding site on the GABAA receptor. DMCM hydrochloride is a benzodiazepine receptor inverse agonist. It binds to the benzodiazepine site on the GABAA receptor complex and allosterically modulates the receptor, reducing the efficacy of GABA-mediated chloride channel opening. This results in decreased inhibitory neurotransmission.
|
|---|---|
| ln Vitro |
DMCM hydrochloride is a potent and selective benzodiazepine inverse agonist. It binds with high affinity to the benzodiazepine site on the GABAA receptor. In vitro, its activity can be assessed by measuring its binding affinity in radioligand binding assays using [3H]-flunitrazepam as a tracer. Its functional effects can be studied by measuring its modulation of GABA-induced chloride influx in oocytes or cells expressing GABAA receptors.
|
| ln Vivo |
Strong anxiogenic, proconvulsant, and convulsant effects are caused by DMCM in the body. In γ2I77 mice, DMCM (20–60 mg/kg; i.p.) has mild anxiolytic-like effects [2].
In vivo, DMCM hydrochloride produces effects opposite to those of benzodiazepines. It is anxiogenic, producing anxiety-like behaviors in animal models, and proconvulsant, lowering the seizure threshold. It can also affect memory and learning. These effects make it a useful tool for studying the role of the GABAA receptor in these processes. |
| Enzyme Assay |
In vitro receptor binding assays for DMCM hydrochloride are performed using membrane preparations from brain tissue or cells expressing GABAA receptors. The compound is incubated with a fixed concentration of a radiolabeled benzodiazepine ligand (e.g., [3H]-flunitrazepam). Nonspecific binding is determined using a benzodiazepine agonist such as diazepam. IC50 or Ki values are calculated from competition binding curves.
|
| Cell Assay |
In vitro cell-based assays for DMCM hydrochloride are performed using cells expressing GABAA receptors. The compound's effect on GABA-induced chloride influx can be measured using electrophysiological techniques (patch-clamp) or by using fluorescent chloride indicators. The compound's inverse agonist activity is demonstrated by its ability to reduce the response to GABA.
|
| Animal Protocol |
Animal/Disease Models: Male γ2I77 mice [2]
Doses: 20 mg/kg and 60 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:Produces moderate anxiolytic-like effects. In vivo animal studies for DMCM hydrochloride are conducted to study its effects on anxiety, seizure susceptibility, and memory. The compound is administered to rodents, and behavioral tests such as the elevated plus maze (for anxiety), the pentylenetetrazol seizure test (for seizure threshold), or the Morris water maze (for memory) are performed. |
| ADME/Pharmacokinetics |
DMCM hydrochloride has a molecular weight of 342.65 and a molecular formula of C15H13Cl2N3 · HCl. As a hydrochloride salt, it is expected to have improved aqueous solubility. It should be stored as powder at -20°C. For in vivo administration, it can be dissolved in saline or other suitable vehicles.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are documented for DMCM hydrochloride in the provided sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound.
|
| References |
|
| Additional Infomation |
See also: ...View more...
DMCM hydrochloride is a benzodiazepine inverse agonist. It is used in research to study the GABAA receptor and its role in anxiety, seizure, and memory. Its effects are opposite to those of benzodiazepine agonists. It is for research use only. |
| Molecular Formula |
C17H19CLN2O4
|
|---|---|
| Molecular Weight |
350.796763658524
|
| Exact Mass |
350.103
|
| CAS # |
1215833-62-7
|
| PubChem CID |
45261899
|
| Appearance |
Light green to green solid powder
|
| LogP |
3.884
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
24
|
| Complexity |
433
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCC1=C2C3=CC(=C(C=C3NC2=CN=C1C(=O)OC)OC)OC.Cl
|
| InChi Key |
FHCRBVQGMZUJKY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H18N2O4.ClH/c1-5-9-15-10-6-13(21-2)14(22-3)7-11(10)19-12(15)8-18-16(9)17(20)23-4;/h6-8,19H,5H2,1-4H3;1H
|
| Chemical Name |
methyl 4-ethyl-6,7-dimethoxy-9H-pyrido[3,4-b]indole-3-carboxylate;hydrochloride
|
| 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 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)
|
| Solubility (In Vitro) |
H2O : ~25 mg/mL (~71.27 mM)
DMSO : ~10 mg/mL (~28.51 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.85 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.85 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 10.0 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 | 2.8506 mL | 14.2531 mL | 28.5063 mL | |
| 5 mM | 0.5701 mL | 2.8506 mL | 5.7013 mL | |
| 10 mM | 0.2851 mL | 1.4253 mL | 2.8506 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
