BAN ORL 24 is a potent and selective NOP (also known as KOR-3) receptor antagonist (IC|50|values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively). BAN ORL 24 Inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca|2+|mobilization in CHO cells|in vitro|and antagonizes NOP agonist-induced reduction in locomotor activity|in vivo|.BAN ORL 24 can is also a brain penetrant.
1.Goto Y, Arai-Otsuki S, Tachibana Y, Ichikawa D, Ozaki S, Takahashi H, Iwasawa Y, Okamoto O, Okuda S, Ohta H et al.. (2006) Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity.. J Med Chem, 49 (3):(847-9). [PMID:16451050]
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