Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists

(2012) David A Sykes et al.   BRITISH JOURNAL OF PHARMACOLOGY

Orexin Receptor Antagonism, a New Sleep-Enabling Paradigm: A Proof-of-Concept Clinical Trial

(2012) P Hoever et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists

(2012) Stefania Faedo et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Orexin receptor antagonism: an ascending multiple-dose study with almorexant

(2012) Petra Hoever et al.   JOURNAL OF PSYCHOPHARMACOLOGY

Orexins and their receptors from fish to mammals: A comparative approach

(2011) Kari K.Y. Wong et al.   GENERAL AND COMPARATIVE ENDOCRINOLOGY

GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo

(2010) DJ Behm et al.   BRITISH JOURNAL OF PHARMACOLOGY

Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia

(2010) Christopher D. Cox et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor

(2009) P Malherbe et al.   BRITISH JOURNAL OF PHARMACOLOGY

Biochemical and Electrophysiological Characterization of Almorexant, a Dual Orexin 1 Receptor (OX1)/Orexin 2 Receptor (OX2) Antagonist: Comparison with Selective OX1 and OX2 Antagonists

(2009) P. Malherbe et al.   MOLECULAR PHARMACOLOGY

A receptor theory-based semimechanistic PD model for the CCR5 noncompetitive antagonist maraviroc

(2008) Philippe Jacqmin et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

The signalling profile of recombinant human orexin-2 receptor

(2008) Jiyou Tang et al.   CELLULAR SIGNALLING

Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor

(2006) Mark R Dowling et al.   BRITISH JOURNAL OF PHARMACOLOGY