A dopamine D3 receptor partial agonist; selectively binds to the dopamine D3 over the D2

BP-897 – 10 mg

Brand:
Cayman
CAS:
314776-92-6
Storage:
-20
UN-No:
Non-Hazardous - /

BP-897 is a dopamine D3 receptor partial agonist.{47754} 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).{47755} 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.{47754}  

 

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Description

A dopamine D3 receptor partial agonist; 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); selective over α1- and α2-adrenergic receptors (Kis = 60 and 83 nM, respectively) and the serotonin 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); increases mitogenesis in NG 108-15 cells with a maximum efficacy of 55%; acts as a dopamine D3 receptor antagonist in a [35S]GTPγS binding assay, inhibiting the effect of dopamine (IC50 = 416.87 nM); reduces cocaine-seeking behavior, but has no reinforcing properties itself, in rats trained to self-administer cocaine at 0.5 and 1 mg/kg

Formal name: N-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-2-naphthalenecarboxamide, monohydrochloride

Synonyms: 

Molecular weight: 454

CAS: 314776-92-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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