| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Targets |
Serotonin 5-HT2 receptors and dopamine D2 receptors. Carbidine selectively inhibits serotonin 5-HT2 receptors in the brain, in contrast to haloperidol and sulpiride which primarily affect dopamine receptors. The trans-isomer of carbidine enhances the biosynthesis of dopamine via blockade of presynaptic autoreceptors on dopaminergic terminals. Carbidine also has adrenomimetic effects by releasing norepinephrine.
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| ln Vitro |
Carbidine exerts its atypical neuroleptic effects primarily through selective inhibition of serotonin 5-HT2 receptors. The compound increases dopamine turnover in frontal cortex, striatum, and hypothalamus to a greater degree than haloperidol, and increases 5-HT turnover in all cerebral regions. The trans-isomer of carbidine is more potent than the cis-isomer in increasing dopamine release. Carbidine also has adrenomimetic effects by releasing norepinephrine, leading to a reduction of endogenous neurotransmitter stores.
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| ln Vivo |
In vivo, carbidine has been studied in animal models for its antipsychotic and antidepressive effects. The compound increases dopamine turnover in frontal cortex, striatum, and hypothalamus to a greater degree than haloperidol, and increases 5-HT turnover in all cerebral regions. The atypical neuroleptic drug carbidine exerts a predominant effect on the frontal cortex, with the serotoninergic component being clearly pronounced. Carbidine has antidepressive properties that may be due to the down-regulation of 5-HT2 receptors in the brain.
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| Enzyme Assay |
In vitro receptor binding assays for carbidine involve measuring the compound's affinity for serotonin 5-HT2 receptors and dopamine D2 receptors using radioligand binding techniques. Membranes from brain tissue or cells expressing the receptors are incubated with radiolabeled ligands and increasing concentrations of carbidine. Bound and free ligand are separated by filtration, and radioactivity is measured. These assays confirm the selective binding of carbidine to 5-HT2 receptors.
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| Cell Assay |
Cellular assays for carbidine involve treating neuronal cells with the compound and measuring neurotransmitter release, receptor binding, or downstream signaling. The compound's effects on dopamine and serotonin turnover can be assessed by measuring neurotransmitter levels in cell culture media. These assays demonstrate the neurochemical effects of carbidine on dopaminergic and serotonergic systems.
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| Animal Protocol |
In vivo animal studies for carbidine typically involve administration to rodents and measurement of monoamine levels and their metabolites in brain structures. Carbidine (25 mg/kg) increases DA turnover in frontal cortex, striatum, and hypothalamus to a greater degree than haloperidol, and increases 5-HT turnover in all cerebral regions. The trans-isomer is more potent than the cis-isomer in increasing dopamine release, as measured by microdialysis in awake rats.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of carbidine are limited and primarily derived from preclinical research. The compound is absorbed following oral or intraperitoneal administration and distributes to the brain. Metabolism and elimination pathways have not been fully characterized. Further pharmacokinetic studies are needed to support clinical development.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of carbidine are limited. As an atypical neuroleptic, the compound's safety profile is expected to be similar to other antipsychotic agents, with potential for extrapyramidal side effects, sedation, and metabolic effects. However, carbidine's selective effects on serotonin receptors may result in a more favorable side effect profile compared to classical neuroleptics like haloperidol.
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| Additional Infomation |
Carbidine is an atypical neuroleptic drug with selective effects on serotonin 5-HT2 receptors and antidepressive properties. Unlike classical neuroleptics, carbidine has a more selective effect on serotonin receptors and increases dopamine turnover to a greater degree than haloperidol. The compound demonstrates stereospecific effects, with the trans-isomer being more potent than the cis-isomer. Carbidine is a research compound that has been studied primarily in preclinical models.
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| Molecular Formula |
C13H20CL2N2
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|---|---|
| Molecular Weight |
275.22
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| Exact Mass |
274.1
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| CAS # |
33162-17-3
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| Related CAS # |
Dicarbine;17411-19-7
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| PubChem CID |
134973
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.043g/cm3
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| Boiling Point |
305.7ºC at 760mmHg
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| Flash Point |
128.8ºC
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| LogP |
3.888
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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 |
0
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| Heavy Atom Count |
17
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| Complexity |
241
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)NC3CCN(C)CC23.Cl.Cl
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| InChi Key |
XWLFAMANDIWUKH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H18N2.2ClH/c1-9-3-4-12-10(7-9)11-8-15(2)6-5-13(11)14-12;;/h3-4,7,11,13-14H,5-6,8H2,1-2H3;2*1H
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| Chemical Name |
2,8-dimethyl-1,3,4,4a,5,9b-hexahydropyrido[4,3-b]indole;dihydrochloride
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| Synonyms |
Carbidine dihydrochloride; Carbidine; Carbidin
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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) |
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 | 3.6335 mL | 18.1673 mL | 36.3346 mL | |
| 5 mM | 0.7267 mL | 3.6335 mL | 7.2669 mL | |
| 10 mM | 0.3633 mL | 1.8167 mL | 3.6335 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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