Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 4, 2010, Pages 1448-1452

  Debenham, John S ^a   Madsen Duggan, Christina B ^a   Toupence, Richard B ^a   Walsh, Thomas F ^a   Wang, Junying ^a   Tong, Xinchun ^a   Kumar, Sanjeev ^a   Lao, Julie ^a   Fong, Tung M ^a   Xiao, Jing Chen ^a   Huang, Cathy R R C ^a   Shen, Chun Pyn ^a   Feng, Yue ^a   Marsh, Donald J ^a   Stribling, D Sloan ^a   Shearman, Lauren P ^a   Strack, Alison M ^a   Goulet, Mark T ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cannabinoid; CB1R; Furopyridine; Inverse agonist; Obesity

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; CANNABINOID 1 RECEPTOR AGONIST; FURO[2,3 B]PYRIDINE DERIVATIVE; TARANABANT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG SYNTHESIS; EXPERIMENTAL DOG; EXPERIMENTAL MONKEY; FOOD INTAKE; HUMAN; IC 50; LIVER MICROSOME; MALE; MOUSE; NONHUMAN; OBESITY; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BENZOPYRANS; DOGS; DRUG DESIGN; FURANS; HAPLORHINI; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MICE, KNOCKOUT; MOLECULAR STRUCTURE; PYRIDINES; RATS; RECEPTOR, CANNABINOID, CB1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 75449091440     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.065     Document Type: Article

References (24)

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18. Feces were not collected.
19. HPLC Log D values were determined at pH 7.3.
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21. Experimental methods were similar to that described in Ref. 10 except 7g was only dosed at 1 and 3 mg/kg based on its improved efficacy.
22. Rats were monitored for 120 h.
23. Discovery Pharmacology services provided by MDS Pharma Services, Taipei, Taiwan.
24. A rotarod test is used to assess the rodent's sensomotor coordination by evaluating how long it can remain on a rotating rod with a steady or increasing rate of rotation.