| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
3-CPMT targets the dopamine transporter (DAT) with high affinity, exhibiting a Ki of 30 nM. It blocks the re-uptake of dopamine by binding to the DAT. The compound's tropane scaffold is responsible for its interaction with the monoamine transporter.
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|---|---|
| ln Vitro |
In cell-free binding assays, 3-CPMT demonstrates high-affinity binding to the dopamine transporter with a Ki of 30 nM. Radioligand displacement studies confirm its potent interaction with the DAT binding site. The compound's affinity for DAT is comparable to that of cocaine, yet its behavioral profile is markedly different. In cellular uptake assays, 3-CPMT potently inhibits dopamine reuptake in neurons. The compound blocks DAT-mediated dopamine transport, leading to increased extracellular dopamine levels. Despite its potent dopamine uptake inhibition, it is a weak psychomotor stimulant and does not produce cocaine-like effects in behavioral models.
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| ln Vivo |
In vivo behavioral studies demonstrate that 3-CPMT does not display a cocaine-like behavioral profile despite its ability to inhibit dopamine uptake. It is a weak psychomotor stimulant and does not substitute for cocaine in addicted rats. This unique profile makes 3-CPMT valuable for understanding the relationship between DAT inhibition and psychostimulant effects.
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| Enzyme Assay |
Dopamine transporter binding assays for 3-CPMT are performed using membrane preparations from cells or tissues expressing DAT. Radioligand binding studies use [³H]WIN 35,428 or similar DAT-selective ligands. Membranes are incubated with varying concentrations of 3-CPMT and the radioligand, followed by filtration and scintillation counting. Ki values are calculated from competition binding curves.
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| Cell Assay |
Dopamine uptake inhibition assays are conducted using neuronal cell cultures or synaptosomal preparations. Cells are pre-incubated with 3-CPMT at various concentrations, then [³H]dopamine is added. Uptake is terminated after a defined period, and accumulated radioactivity is measured. IC50 or Ki values are determined from concentration-response curves.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 3-CPMT have been characterized in rodent models. The compound is capable of crossing the blood-brain barrier due to its lipophilic nature. Its long-acting antihistaminic properties suggest extended duration of action. Detailed PK parameters including half-life and bioavailability require further characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies on 3-CPMT are limited. In behavioral studies, the compound is administered at various doses without significant adverse effects reported. Its weak psychomotor stimulant profile suggests a lower abuse liability compared to cocaine. The compound's antihistaminic activity may contribute to its safety profile.
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| References |
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| Additional Infomation |
3-CPMT is a cocaine analog that binds with a high affinity to the dopamine transporter and blocks the reabsorption of dopamine.
3-CPMT is a research tool for studying dopamine transporter function and the mechanisms of psychostimulant action. Its unique property of inhibiting dopamine uptake without producing cocaine-like effects makes it valuable for understanding the dissociation between DAT inhibition and behavioral stimulation. The compound is also known for its antihistaminic activity. |
| Molecular Formula |
C21H25CL2NO
|
|---|---|
| Molecular Weight |
378.34
|
| Exact Mass |
377.131
|
| CAS # |
14008-79-8
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| PubChem CID |
203135
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
437.2ºC at 760mmHg
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| Flash Point |
218.2ºC
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| Vapour Pressure |
7.62E-08mmHg at 25°C
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| LogP |
5.811
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.ClC1C=CC(C(OC2CC3CCC(N3C)C2)C2C=CC=CC=2)=CC=1
|
| InChi Key |
FXKCQWIUITUJFU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H24ClNO.ClH/c1-23-18-11-12-19(23)14-20(13-18)24-21(15-5-3-2-4-6-15)16-7-9-17(22)10-8-16;/h2-10,18-21H,11-14H2,1H3;1H
|
| Chemical Name |
3-[(4-chlorophenyl)-phenylmethoxy]-8-methyl-8-azabicyclo[3.2.1]octane;hydrochloride
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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 | 2.6431 mL | 13.2156 mL | 26.4313 mL | |
| 5 mM | 0.5286 mL | 2.6431 mL | 5.2863 mL | |
| 10 mM | 0.2643 mL | 1.3216 mL | 2.6431 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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