Selective CB2 receptor agonists. Part 3: The optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 3, 2015, Pages 587-592

  Bartolozzi, Alessandra ^a   Cirillo, Pier Francesco ^a   Berry, Angela K ^a   Hickey, Eugene R ^a   Thomson, David S ^a   Wu, Lifen ^a   Zindell, Renee ^a   Albrecht, Claudia ^c   Ceci, Angelo ^b   Gemkow, Mark J ^c   Nagaraja, Nelamangala V ^a   Romig, Helmut ^b   Sauer, Achim ^b   Riether, Doris ^b  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

^c EVOTEC AG   (Germany)

Author keywords

Cannabinoid receptor; CB1; CB2; Metabolic stability; Piperidine; Solubility

Indexed keywords

CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR AGONIST; CYCLIC AMP; DULOXETINE; PIPERIDINE DERIVATIVE; CANNABINOID 2 RECEPTOR; LIGAND; PIPECOLIC ACID DERIVATIVE; PIPERIDINE; PROTEIN BINDING; THIAZINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STABILITY; HUMAN; HUMAN TISSUE; HYPERALGESIA; IN VIVO STUDY; NEUROPATHIC PAIN; NONHUMAN; PHARMACOPHORE; PHYSICAL CHEMISTRY; PROCESS OPTIMIZATION; RAT; STREPTOZOTOCIN-INDUCED DIABETIC NEUROPATHY; STRUCTURE ACTIVITY RELATION; AGONISTS; ANIMAL; CHEMICALLY INDUCED; CHEMISTRY; DIABETIC NEUROPATHIES; HALF LIFE TIME; LIVER MICROSOME; MALE; METABOLISM; PAIN; SOLUBILITY; WISTAR RAT;

RATTUS;

ANIMALS; DIABETIC NEUROPATHIES; HALF-LIFE; HUMANS; LIGANDS; MALE; MICROSOMES, LIVER; PAIN; PIPECOLIC ACIDS; PIPERIDINES; PROTEIN BINDING; RATS; RATS, WISTAR; RECEPTOR, CANNABINOID, CB1; RECEPTOR, CANNABINOID, CB2; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZINES;

EID: 84920865262     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.12.031     Document Type: Article

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