Non-basic ligands for aminergic GPCRs: The discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 12, 2010, Pages 3708-3712

  Ladduwahetty, Tammy ^a,b   Gilligan, Myra ^a   Humphries, Alexander ^a   Merchant, Kevin J ^a   Fish, Rebecca ^a   McAlister, George ^a   Ivarsson, Magnus ^a   Dominguez, Maria ^a   O'Connor, Desmond ^a   MacLeod, Angus M ^a,b  

^a Merck Sharp & Dohme Limited   (United Kingdom)

^b BioFocus DPI   (United Kingdom)

Author keywords

5 HT2A; Diaryl sulfones; GPCRs; Non basic

Indexed keywords

AMINE; DIAZEPAM; G PROTEIN COUPLED RECEPTOR; M 1009013; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN 2C RECEPTOR; SULFONE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG ADSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; HYDROGENATION; IN VITRO STUDY; MALE; NONHUMAN; PHYSICAL CHEMISTRY; PROTON TRANSPORT; RAT; RHESUS MONKEY; SLEEP DISORDER;

ADMINISTRATION, ORAL; AMINES; ANIMALS; BIOLOGICAL AVAILABILITY; DRUG DISCOVERY; HUMANS; LIGANDS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, G-PROTEIN-COUPLED; SEROTONIN AGONISTS; SLEEP DISORDERS; SULFONES;

EID: 77954213384     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.090     Document Type: Article

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