| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
bPiDDB targets neuronal nicotinic acetylcholine receptors (nAChRs), especially those containing the α6β2 subunits. It acts as an antagonist at these receptors, inhibiting nicotine-induced dopamine release. This selectivity for α6β2-containing nAChRs makes it a valuable tool for studying the role of these receptor subtypes in addiction and other neurological processes.
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| ln Vitro |
bPiDDB is a potent nAChR antagonist with an IC50 of 2 nM. It inhibits nicotine-induced striatal dopamine (DA) release by interacting with α6β2-containing nAChRs. This potent inhibition of dopamine release is central to its mechanism of action and its utility in studying nicotinic receptor function and dopaminergic signaling pathways.
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| ln Vivo |
When given peripherally, bPiDDB suppresses the release of dopamine (DA) in the nucleus accumbens in response to nicotine, which lessens the addiction potential of nicotine in rats [1]. Following peripheral injection, bPiDDB is bioavailable to the brain and is actively transported by blood-brain barrier choline transporters to the central compartment [1].
When given peripherally, bPiDDB suppresses the release of dopamine (DA) in the nucleus accumbens in response to nicotine, which lessens the addiction potential of nicotine in rats. Following peripheral injection, bPiDDB is bioavailable to the brain and is actively transported by blood-brain barrier choline transporters to the central compartment. This demonstrates its ability to cross the blood-brain barrier and exert central effects. |
| Enzyme Assay |
For non-cell-based receptor binding assays, bPiDDB can be evaluated using membrane preparations from cells expressing α6β2 nAChRs. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-epibatidine. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled nicotine. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing α6β2 nAChRs are cultured in appropriate media. For functional assays, dopamine release is measured in striatal slices or synaptosomal preparations. Tissues are pre-loaded with [3H]-dopamine and then stimulated with nicotine in the presence or absence of various concentrations of bPiDDB. The amount of [3H]-dopamine released is measured by liquid scintillation counting. The reduction in dopamine release compared to control indicates antagonist activity. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, bPiDDB can be administered to rats via peripheral injection. In models of nicotine addiction, the compound's ability to suppress nicotine-induced dopamine release in the nucleus accumbens is assessed using microdialysis. The compound's effect on addiction-related behaviors, such as self-administration or conditioned place preference, can also be evaluated. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
bPiDDB has a molecular formula of C24H38Br2N2 and a molecular weight of 514.38. It is soluble in DMSO at 100 mg/mL (194.41 mM). The compound should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for 6 months. Following peripheral injection, it is bioavailable to the brain and is actively transported across the blood-brain barrier by choline transporters.
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| Toxicity/Toxicokinetics |
The toxicity profile of bPiDDB has not been extensively reported. As a potent nAChR antagonist, potential adverse effects may include modulation of cholinergic signaling, which could affect various physiological processes. 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 | |
| Additional Infomation |
bPiDDB (CAS 525596-66-1) is a potent nAChR antagonist that inhibits nicotine-induced dopamine release by interacting with α6β2-containing nAChRs. It is widely used in neuroscience and addiction research to study nicotinic receptor subtype function, dopaminergic signaling, and the development of novel therapeutic strategies for nicotine dependence. It is available for research purposes only.
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| Molecular Formula |
C24H38BR2N2
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| Molecular Weight |
514.38
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| Exact Mass |
512.14
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| CAS # |
525596-66-1
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| PubChem CID |
9983961
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| Appearance |
Off-white to light yellow ointment
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
28
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| Complexity |
298
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C[N+](=CC=C1)CCCCCCCCCCCC[N+]2=CC=CC(=C2)C.[Br-].[Br-]
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| InChi Key |
NNPBJCAIRCFEFZ-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C24H38N2.2BrH/c1-23-15-13-19-25(21-23)17-11-9-7-5-3-4-6-8-10-12-18-26-20-14-16-24(2)22-26;;/h13-16,19-22H,3-12,17-18H2,1-2H3;2*1H/q+2;;/p-2
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| Chemical Name |
3-methyl-1-[12-(3-methylpyridin-1-ium-1-yl)dodecyl]pyridin-1-ium;dibromide
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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) |
DMSO: 100 mg/mL (194.41 mM)
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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 | 1.9441 mL | 9.7204 mL | 19.4409 mL | |
| 5 mM | 0.3888 mL | 1.9441 mL | 3.8882 mL | |
| 10 mM | 0.1944 mL | 0.9720 mL | 1.9441 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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