Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 1, 2011, Pages 506-509

  Morrison, Angus J ^a   Adam, Julia M ^a   Baker, James A ^a   Campbell, Robert A ^a   Clark, John K ^a   Cottney, Jean E ^a   Deehan, Maureen ^a   Easson, Anna Marie ^a   Fields, Ruth ^a   Francis, Stuart ^a   Jeremiah, Fiona ^a   Keddie, Neil ^a   Kiyoi, Takao ^a   McArthur, Duncan R ^a   Meyer, Karsten ^a   Ratcliffe, Paul D ^a   Schulz, Jurgen ^a   Wishart, Grant ^a   Yoshiizumi, Kazuya ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cannabinoid; CB1 receptor; GPCR agonist

Indexed keywords

2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; AMIDE; CANNABINOID 1 RECEPTOR AGONIST; HETEROCYCLIC COMPOUND; INDOLE DERIVATIVE; PIPERAZINE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG ELIMINATION; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG STABILITY; DRUG SYNTHESIS; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; TAIL FLICK TEST; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; DRUG DESIGN; HETEROCYCLIC COMPOUNDS; INDOLES; MICE; MICROSOMES; MODELS, MOLECULAR; RECEPTOR, CANNABINOID, CB1; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

EID: 78650515320     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.093     Document Type: Article

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15. max data were then compared between groups using the Kruskal-Wallis one-way analysis of variance, a non-parametric statistical test. If statistical significance (P <0.05) was observed with this test, the vehicle group and each of the treatment groups were compared using the non-parametric Dunn's test (Unistat 5.0 software).