Potent and selective, sulfamide-based human β3-adrenergic receptor agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 12, 2004, Pages 3235-3240

  Dow, Robert L ^a   Paight, Ernest S ^a   Schneider, Steven R ^a   Hadcock, John R ^a   Hargrove, Diane M ^a   Martin, Kelly A ^a   Maurer, Tristan S ^a   Nardone, Nancy A ^a   Tess, David A ^a   DaSilva Jardine, Paul ^a  

^a PFIZER INC   (United States)

Author keywords

3 Adrenergic receptor; Agonist; Sulfamide

Indexed keywords

BETA 3 ADRENERGIC RECEPTOR STIMULATING AGENT; L 796568; UNCLASSIFIED DRUG;

ADULT; AGONIST; ARTICLE; BINDING AFFINITY; BODY COMPOSITION; CHRONIC DRUG ADMINISTRATION; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; ENERGY EXPENDITURE; HUMAN; LIPOPHILICITY; MALE; MOLECULAR WEIGHT; NORMAL HUMAN; PHARMACOPHORE; RECEPTOR INTRINSIC ACTIVITY; REDUCTION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ADRENERGIC BETA-AGONISTS; ANIMALS; HUMANS; OXYGEN CONSUMPTION; RATS; RECEPTORS, ADRENERGIC, BETA-3; SULFONAMIDES;

EID: 2442462015     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.03.089     Document Type: Article

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18. ″ ). The system is calibrated and the run started (8:00-8:30 am). Oxygen consumption measurements are made every 10 min for 3 h, at which time the animals are dosed with test compounds (17j dosed as the monotosylate salt) or vehicle ( n =4 each). Oxygen consumption measurements continue for 2 h. Oxygen consumption values associated with periods of high ambulatory activity (>100 counts/10 min) are excluded from all calculations, as well as the first 5 values of the run and the first value after dosing (settle-down periods)