| Identification | Back Directory | [Name]
BP 897 | [CAS]
314776-92-6 | [Synonyms]
BP897/BP-897
BP897 >98% (HPLC), solid
N-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]naphthalene-2-carboxamide
N-[4-[4-(2-Methoxyphenyl)-1-piperazinyl]butyl]-2-naphthalenecarboxamide monohydrochloride | [Molecular Formula]
C26H31N3O2 | [MDL Number]
MFCD04039996 | [MOL File]
314776-92-6.mol | [Molecular Weight]
417.55 |
| Hazard Information | Back Directory | [Description]
BP-897 is a dopamine D3 receptor partial agonist. It selectively binds to the dopamine D3 over the D2, D1, and D4 receptors (Kis = 0.92, 61, 3,000, and 300 nM, respectively, for the recombinant human receptors). It is also selective over α1- and α2-adrenergic receptors (Kis = 60 and 83 nM, respectively) and the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT7 (Kis = 84 and 345 nM, respectively), as well as muscarinic, histamine, and opioid receptors (Kis = >1 μM for all). BP-897 inhibits cAMP accumulation induced by forskolin (EC50 = 1 nM) and increases mitogenesis in NG 108-15 cells with a maximum efficacy of 55%, an effect that can be blocked by the dopamine D3 receptor antagonist nafadotride. It also acts as a dopamine D3 receptor antagonist, failing to increase [35S]GTPγS binding to CHO cell membranes expressing the recombinant human D3 receptor and inhibiting the effect of dopamine in the same assay (IC50 = 416.87 nM). BP-897 (0.5 and 1 mg/kg) reduces cocaine-seeking behavior, but has no reinforcing properties itself, in rats trained to self-administer cocaine. | [Uses]
BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM)[1]. | [Biochem/physiol Actions]
Partially selective D3 dopamine receptor agonist. | [in vivo]
BP 897 hydrochloride 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[1]. | Animal Model: | Male Listar hooded rats[1] | | Dosage: | 0.05, 0.5, 1 mg/kg | | Administration: | i.p.; 30 min before the session | | Result: | Reduced cocaine-seeking behaviour 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. |
| [IC 50]
D2 Receptor; D3 Receptor | [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. DOI:10.1038/22560 |
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Sigma-Aldrich
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