Description |
BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 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). BP 897 exhibits selective inhibition of cocaine-seeking behavior[1].
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Related Catalog |
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In Vitro |
BP 897 also displays low affinities at D1 and D4 receptors (Ki=3 and 0.3 μM, respectively), as well as at α1 and α2 adrenergic receptors (Ki=60 and 83 nM, respectively), 5HT1A and 5HT7 receptors (Ki=84 and 345 nM, respectively), and negligible affinities (Ki>1 μM) atmuscarinic, histamine and opiate receptors[1]. In NG 108-15 cells expressing the human D3 receptor, BP 897 inhibits forskolin-induced cyclic AMP accumulation with an EC50 of 1 nM. BP 897 activates mitogenesis and this response is antagonized by the preferential D3 receptor antagonist Nafadotride (1 μM). BP 897 also partially antagonized the response induced by quinpirole (10 nM)[1].
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In Vivo |
BP 897 (0.05, 0.5, 1 mg/kg; i.p.; 30 min before the session) reduces 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[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.
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References |
[1]. Pilla M, et al. Selective inhibition of cocaine-seeking behaviour by a partial dopamine D3 receptor agonist [published correction appears in Nature 1999 Sep 23;401(6751):403]. Nature. 1999;400(6742):371-375.
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