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| Cas No.: | 314776-92-6 |
| Chemical Name: | 2-Naphthalenecarboxamide,N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-, hydrochloride (1:1) |
| Synonyms: | 2-Naphthalenecarboxamide,N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-, hydrochloride (1:1);BP897;N-{4-[4-(2-Methoxyphenyl)-1-piperazinyl]butyl}-2-naphthamide hydr ochloride (1:1);N-{4-[4-(2-Methoxyphenyl)piperazin-1-yl]butyl}-2-naphthamide hydrochloride (1:1);N-[4-(4-(2-Methoxyphenyl)piperazinyl)butyl]-2-naphthamide;BP 897 |
| SMILES: | COC1C(=CC=CC=1)N2CCN(CCCCNC(=O)C3C=C4C(C=CC=C4)=CC=3)CC2 |
| Formula: | C26H31N3O2 |
| M.Wt: | 417.54324 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with Kis of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (Kis, 3 and 0.3 µM, respectively). |
| Target: | Ki: 0.92 nM (D3 receptor), 61 nM (D2 receptor), 0.3 µM (D4 receptor), 3 µM (D1 receptor)[1]. |
| In Vivo: | BP 897 binds to D2-receptor in mouse striatum with an ED50 of 15 mg/kg, and the D3-receptor occupancy is blow 0.5 mg/kg. BP 897 (0, 0.05, 0.5, 1 mg/kg) inhibits cocaine-seeking behaviour that depends upon the presentation of drug-associated cues, without having any intrinsic, primary rewarding effects[1]. |
| In Vitro: | BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with a Ki of 0.92 nM for D3 receptor, a 70 times lower affinity at the D2 receptor (Ki, 61 nM), and shows low affinities at D1 and D4 receptors (Ki = 3 and 0.3 µM, respectively). BP 897 also weakly binds to α1 and α2 adrenergic receptors (Ki = 60 and 83 nM, respectively), 5HT1A and 5HT7 receptors (Ki = 84 and 345 nM, respectively), and has negligible affinities (Ki > 1 µM) at muscarinic, histamine and opiate receptors. BP 897 inhibits forskolin-induced cyclic AMP accumulation with an EC50 of 1.0 ± 0.3 nM, and increases mitogenesis, another D3-receptor-mediated response (EC50 = 3 ± 1 nM) in NG 108-15 cells expressing the human D3 receptor. However, BP 897 (1 µM) does not inhibit cyclic AMP accumulation or trigger mitogenesis in cells expressing the D2 receptor[1]. |
| References: | [1]. Pilla M, et al. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist. Nature. 1999 Jul 22;400(6742):371-5. |