Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs)

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 24, 2013, Pages 6620-6624

  Mercer, Swati P ^a   Roecker, Anthony J ^a   Garson, Susan ^a   Reiss, Duane R ^a   Meacham Harrell, C ^a   Murphy, Kathy L ^a   Bruno, Joseph G ^a   Bednar, Rodney A ^a   Lemaire, Wei ^a   Cui, Donghui ^a   Cabalu, Tamara D ^a   Tang, Cuyue ^a   Prueksaritanont, Thomayant ^a   Hartman, George D ^a   Young, Steven D ^a   Winrow, Christopher J ^a   Renger, John J ^a   Coleman, Paul J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Hypocretin; Insomnia; Orexin receptor antagonists; Rat sleep EEG; Selective orexin 2 receptor antagonists

Indexed keywords

2,5 DIARYLNICOTINAMIDE DERIVATIVE; ALMOREXANT; FILOREXANT; HYPNOTIC SEDATIVE AGENT; JNJ 10397049; NICOTINAMIDE DERIVATIVE; OREXIN; OREXIN 2 RECEPTOR; OREXIN 2 RECEPTOR ANTAGONIST; SB 649868; SUVOREXANT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING ASSAY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ELECTROENCEPHALOGRAPHY; HIGH THROUGHPUT SCREENING; NONHUMAN; PRIMARY INSOMNIA; RAT; REACTION ANALYSIS; RECEPTOR AFFINITY; SLEEP INDUCTION;

PORZANA; RATTUS;

HYPOCRETIN; INSOMNIA; OREXIN RECEPTOR ANTAGONISTS; RAT SLEEP EEG; SELECTIVE OREXIN-2 RECEPTOR ANTAGONISTS;

ANIMALS; DOGS; DRUG EVALUATION, PRECLINICAL; HALF-LIFE; HUMANS; NICOTINIC ACIDS; OREXIN RECEPTORS; PROTEIN BINDING; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84888874211     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.10.045     Document Type: Article

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