314776-92-6

BP-897 is a dopamine D₃ receptor partial agonist. It selectively binds to the dopamine D₃ over the D₂, D₁, and D₄ receptors (K_is = 0.92, 61, 3,000, and 300 nM, respectively, for the recombinant human receptors). It is also selective over α₁- and α₂-adrenergic receptors (K_is = 60 and 83 nM, respectively) and the serotonin (5-HT) receptor subtypes 5-HT_1A and 5-HT₇ (K_is = 84 and 345 nM, respectively), as well as muscarinic, histamine, and opioid receptors (K_is = >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.

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].

Partially selective D3 dopamine receptor agonist.

D₂ Receptor; D₃ Receptor

[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