BP-897

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 alpha1- and alpha2-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]GTPgammaS 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.Formal Name: N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-naphthalenecarboxamide, monohydrochloride. CAS Number: 314776-92-6. Molecular Formula: C26H31N3O2 . HCl. Formula Weight: 454.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5mg/mL, DMF:PBS (pH 7.2) (1:2): 0.3mg/mL, DMSO: 2mg/mL, Ethanol: 2mg/mL. lambdamax: 232, 281 nm. SMILES: O=C(NCCCCN1CCN(C2=C(OC)C=CC=C2)CC1)C3=CC4=CC=CC=C4C=C3.Cl. InChi Code: InChI=1S/C26H31N3O2.ClH/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),1H. InChi Key: KFWJGUZIZAPFMX-UHFFFAOYSA-N.