Potent and selective non-peptide orexin OX1
receptor antagonist (Kd
= 3.76 nM). Exhibits 100-fold selectivity for OX1
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
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Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function.
Ellis et al.
Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Langmead et al.