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Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 18, 2011, Pages 5562-5567

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders

(23) Di Fabio, Romano a Pellacani, Annalisa a Faedo, Stefania a Roth, Adelheid a Piccoli, Laura a Gerrard, Philip a Porter, Rod A b Johnson, Christopher N b Thewlis, Kevin b Donati, Daniele a Stasi, Luigi a Spada, Simone a Stemp, Geoffrey b Nash, David b Branch, Clive b Kindon, Leanda b Massagrande, Mario a Poffe, Alessandro a Braggio, Simone a Chiarparin, Elisabetta a more..

a GSK (Italy)

b GLAXOSMITHKLINE (United Kingdom)

Author keywords

Central nervous system (CNS); Conformational analysis; G Protein coupled receptor (GPCR); Hypnotic agent; Orexin receptor antagonist; Sleep disorders; Structure activity relationship (SAR)

Indexed keywords

ALMOREXANT; OREXIN 1 RECEPTOR; OREXIN 1 RECEPTOR ANTAGONIST; OREXIN 2 RECEPTOR; OREXIN 2 RECEPTOR ANTAGONIST; PIPERIDINE DERIVATIVE; SB 649868; UNCLASSIFIED DRUG; ZOLPIDEM;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG CONFORMATION; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG METABOLISM; GROOMING; HUMAN; HUMAN CELL; HYPNOSIS; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; SLEEP DISORDER; SLEEP PATTERN; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PIPERIDINES; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NEUROPEPTIDE; SLEEP DISORDERS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 80051923847 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2011.06.086 Document Type: Article

Times cited : (47)

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