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Purity: ≥98%
BP 897 is a first potent and selective agonist of dopamine D3 receptor, and a weak antagonist of dopamine D2 receptor with Kis of 0.92 nM and 61 nM for D3 and D2 receptors. It exhibits low affinities, with Ki values of 3 and 0.3 µM at the D1 and D4 receptors, respectively. In vitro, BP 897 functions as a partial agonist and can take on an antagonistic role in vivo. Without any intrinsic, primary rewarding effects, BP 897 inhibits cocaine-seeking behavior that is dependent on the presentation of drug-associated cues. According to the data, substances such as BP 897 may be used to lessen drug cravings and relapse susceptibility that are brought on by environmental cues related to drug use.
| Targets |
D2 Receptor; D3 Receptor
BP897: Dopamine D3 receptor (Receptors, Dopamine D3) [1] |
|---|---|
| ln Vitro |
BP 897 hydrochloride adsorbs D1 and D4 (Ki=3 μM and 0.3 μM), α1 and α2 addin energy adsorption (Ki=60 nM and 83 nM) and 5HT1A and 5HT7 adsorption (Ki=84 nM and 345 nM) ) has affinity; it has negligible affinity for muscarinic, histamine and opioid receptors (Ki>1 μM)[1]. BP 897 hydrochloride inhibits forskolin-induced cyclic AMP accumulation in NG 108-15 cells expressing human D3 receptor with EC50=1 nM. BP 897 hydrochloride activates mitogenesis, and this response is preferentially induced by the D3 monoclonal antibody Nafadotride (1 μM) monoclonal antibody. BP 897 hydrochloride is also partially resistant to quinpirole (10 nM)-induced responses [1].
1. BP897 is identified as the first D3-receptor-selective agonist, verified by in vitro assays with recombinant dopamine receptors (D1, D2, D3), and it acts as a partial agonist at the dopamine D3 receptor in vitro [1] 2. In CHO cell lines transfected with dopamine receptor expression vectors, BP897 exhibits selective binding and activation activity towards the dopamine D3 receptor, with no significant selective agonistic or antagonistic effects on dopamine D1 and D2 receptors [1] |
| ln Vivo |
BP 897 hydrochloride binds to D2 capture in the mouse striatum with an ED50 of 15 mg/kg and a D3 capture occupancy of less than 0.5 mg/kg[1]. Animal model: Male Listar hooded rat [1] Dosage: 0.05, 0.5, 1 mg/kg Administration: intraperitoneal injection; 30 minutes before treatment Results: Dose-dependent reduction in cocaine-seeking behavior prior to first infusion of cocaine, Doses were similar to those at which BP 897 responded to rotation and c-fos expression.
1. In mice with disrupted D3-receptor genes (D3 receptor knockout mice) and wild-type mice, BP897 is confirmed to exert its pharmacological effects by targeting the dopamine D3 receptor; it does not produce any intrinsic, primary rewarding effects in vivo [1] 2. In rat (Wistar rat) models of cocaine-seeking behaviour, BP897 selectively inhibits cocaine-seeking behaviour induced by drug-associated environmental stimuli, without interfering with the animals' natural reward-related behaviours [1] 3. BP897 can reduce the motivational effects of cocaine-related cues in vivo, and its action either as an agonist or an antagonist at the dopamine D3 receptor contributes to the inhibition of relapse vulnerability to cocaine addiction [1] |
| Enzyme Assay |
1. Recombinant dopamine receptor binding and activation assay: Construct experimental systems expressing recombinant dopamine D1, D2, and D3 receptors, incubate BP897 with different recombinant receptors, and detect the downstream signalling pathway indicators of receptor activation (e.g., cAMP levels) to evaluate the binding and activation ability of BP897 to different dopamine receptors, thereby determining its selectivity for the D3 receptor [1]
2. Receptor extract binding assay: Prepare receptor extracts from tissue samples of D3 receptor knockout mice and wild-type mice, incubate with BP897, and measure the binding affinity of BP897 to endogenous dopamine receptors to verify its selective binding characteristics to the D3 receptor [1] |
| Cell Assay |
1. CHO cell-based dopamine receptor activity assay: Transfect CHO cells with expression vectors of dopamine D1, D2, and D3 receptors respectively, culture the cells to reach the logarithmic growth phase, then add BP897 at different concentrations to the cell culture system. After a certain incubation time, detect the changes in intracellular second messenger (e.g., cyclic adenosine monophosphate, cAMP) levels using relevant detection methods, and analyse the agonistic activity of BP897 on different dopamine receptors to confirm its property as a partial agonist of the D3 receptor [1]
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| Animal Protocol |
Male Listar hooded rats
0.05, 0.5, 1 mg/kg i.p.; 30 min before the session 1. Experimental animals and grouping: Male Wistar rats and mice (including D3 receptor knockout mice and wild-type mice) are used as experimental subjects; the animals are randomly divided into a control group (administered with normal saline or blank solvent) and a BP897 treatment group, with multiple dose subgroups set according to experimental needs [1] 2. Cocaine-seeking behaviour model establishment: First, train the animals for cocaine self-administration to establish a stable cocaine-seeking behaviour model, in which the animals learn to associate specific environmental cues with cocaine rewards (e.g., pressing a lever to obtain cocaine) [1] 3. Drug administration and behavioural observation: After model establishment, BP897 is administered to the treatment group (the specific administration route and frequency are not reported in the literature), and the control group is given the corresponding solvent. Then, the animals are exposed to cocaine-associated environmental cues, and the behavioural indicators of cocaine-seeking (e.g., the number of active lever presses by the animals) are recorded and statistically analysed over a specific period to evaluate the inhibitory effect of BP897 on cocaine-seeking behaviour [1] 4. Validation experiment with knockout mice: The same cocaine-seeking behaviour experiment is conducted on D3 receptor knockout mice and wild-type mice treated with BP897, and the behavioural differences between the two groups are compared to confirm that the pharmacological effect of BP897 is dependent on the dopamine D3 receptor [1] |
| References | |
| Additional Infomation |
1. BP897 is the first designed selective dopamine D3 receptor agonist. In vitro, it acts as a partial agonist, while in vivo, it can function as either an agonist or an antagonist [1]. 2. The mechanism of action of BP897 is to target the dopamine D3 receptor, reduce the motivational effect of drug-related environmental stimuli, thereby inhibiting cocaine craving behavior and the risk of relapse of cocaine addiction [1]. 3. BP897 itself does not have a direct reward effect, avoiding the risk of drug abuse, and is a potential candidate drug for the treatment of cocaine addiction (and related diseases) [1]. 4. Pharmacological, autopsy and genetic studies have shown that the dopamine D3 receptor is closely related to drug addiction, and the development of BP897 is based on this. It provides an experimental basis for the clinical treatment of drug addiction targeting the dopamine D3 receptor [1].
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| Molecular Formula |
C26H31N3O2
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|---|---|
| Molecular Weight |
417.54324
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| Exact Mass |
453.218
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| Elemental Analysis |
C, 74.79; H, 7.48; N, 10.06; O, 7.66
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| CAS # |
314776-92-6
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| Related CAS # |
BP 897; 192384-87-5
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| PubChem CID |
3038494
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| Appearance |
Solid powder
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| Boiling Point |
654.5ºC at 760mmHg
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| Flash Point |
349.6ºC
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| LogP |
5.56
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)C=C3)=O)CC2)C=CC=C1.[H]Cl
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| InChi Key |
MNHDKMDLOJSCGN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31N3O2/c1-31-25-11-5-4-10-24(25)29-18-16-28(17-19-29)15-7-6-14-27-26(30)23-13-12-21-8-2-3-9-22(21)20-23/h2-5,8-13,20H,6-7,14-19H2,1H3,(H,27,30)
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| Chemical Name |
N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-2-naphthamide
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| Synonyms |
BP-897; BP897; BP 897
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~125 mg/mL (~275.33 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 | 2.3950 mL | 11.9749 mL | 23.9498 mL | |
| 5 mM | 0.4790 mL | 2.3950 mL | 4.7900 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3950 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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