| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Targets |
D2 Receptor D3 Receptor
BP 897 targets the dopamine D3 receptor as a partial agonist and the D2 receptor as a weak antagonist. It shows high affinity for the D3 receptor (Ki=0.92 nM) and significantly lower affinity for the D2 receptor (Ki=61 nM). This selectivity makes it a valuable tool for studying D3 receptor function. |
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| ln Vitro |
BP 897 has activity against the following receptor types: α1 and α2 adrenergic (Ki = 60 nM and 83 nM), D1 and D4 (Ki = 3 μM and 0.3 μM), and 5HT1A and 5HT7 (Ki = 84 nM and 345 nM). Has a little affinity (Ki>1 μM) for opioid, histamine, and muscarinic receptors [1]. In NG 108-15 cells expressing human D3 receptors, BP 897 suppresses forskolin-induced cyclic AMP buildup with EC50=1 nM. BP 897 also promotes mitogenesis, a response that is specifically inhibited by the D3 receptor antagonist Nafadotride (1 μM). Additionally, quinpirole (10 nM)-induced reactions are partially attenuated by BP 897 [1].
In cell-free receptor binding assays, BP 897 demonstrates high affinity for the dopamine D3 receptor with a Ki of 0.92 nM. It has a 70-fold lower affinity for the D2 receptor (Ki=61 nM). Its activity as a partial agonist at D3 and antagonist at D2 is confirmed in functional assays. Cellular functional assays demonstrate that BP 897 activates mitogenesis, and this response is antagonized by the preferential D3 receptor antagonist nafadotride. It also partially antagonizes the response induced by quinpirole (10 nM). These results confirm its partial agonist activity at D3 and weak antagonist activity at D2. |
| ln Vivo |
In vivo, BP 897 exhibits selective inhibition of cocaine-seeking behavior. This effect is attributed to its action at the dopamine D3 receptor. The compound's unique profile of D3 partial agonism and D2 weak antagonism makes it a promising candidate for the treatment of addiction and other neuropsychiatric disorders.
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| Enzyme Assay |
Cell-free receptor binding assays for BP 897 are performed using membrane preparations from cells expressing human dopamine D2 and D3 receptors. Radioligand displacement studies use [³H]spiperone or other D2/D3-selective ligands. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cellular functional assays for BP 897 are conducted using cells expressing the dopamine D3 receptor. The compound's partial agonist activity is assessed by its ability to activate D3 receptor-mediated signaling, such as mitogenesis. Its antagonist activity at D2 is assessed by its ability to inhibit quinpirole-induced responses.
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| Animal Protocol |
Animal/Disease Models: Male Listar hooded rats[1]
Doses: 0.05, 0.5, 1 mg/kg Route of Administration: ip; 30 min before the session Experimental Results: decreased cocaine-seeking behavior before the first infusion of cocaine, in a dose-dependent manner, at doses similar to those at which BP 897 produced its responses on rotations and c-fos expression. In vivo studies for BP 897 are conducted in animal models of addiction, such as cocaine self-administration models. The compound's ability to inhibit drug-seeking behavior is assessed. These studies confirm its potential as a therapeutic agent for addiction. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of BP 897 are not extensively reported in the available literature. As a small-molecule D3 receptor ligand, it is expected to be capable of crossing the blood-brain barrier.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for BP 897 are limited. As a research compound, comprehensive toxicological evaluations would be necessary for its development as a therapeutic agent.
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| References |
[1]. Pilla M, et al. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist [published correction appears in Nature 1999 Sep 23;401(6751):403]. Nature. 1999;400(6742):371-375.
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| Additional Infomation |
N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-naphthoamide is a naphthoamide.
BP 897 is a research compound with potential applications in the treatment of addiction and neuropsychiatric disorders. Its selective partial agonism at the D3 receptor and weak antagonism at D2 make it a valuable tool for studying dopamine receptor function. It is not approved for clinical use. |
| Molecular Formula |
C26H31N3O2
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|---|---|
| Molecular Weight |
417.54324
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| Exact Mass |
417.241
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| CAS # |
192384-87-5
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| Related CAS # |
BP 897 hydrochloride;314776-92-6
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| PubChem CID |
3038495
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
654.5±55.0 °C at 760 mmHg
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| Flash Point |
349.6±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
4.52
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3
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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]naphthalene-2-carboxamide
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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 | 2.3950 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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