Chemical Name: [5-(2-Fluorophenyl)-2-methyl-4-thiazolyl][2(S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl-1-pyrrolidinyl]methanone
Biological ActivityPotent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM). Exhibits 100-fold selectivity for OX1 over OX2 receptors. Has no effect at serotonergic, dopaminergic, adrenergic or purinergic receptors. Inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Langmead et al.
Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function.
Ellis et al.
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