Your browser doesn't support javascript.
loading
Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.
Bartolozzi, Alessandra; Cirillo, Pier Francesco; Berry, Angela K; Hickey, Eugene R; Thomson, David S; Wu, Lifen; Zindell, Renee; Albrecht, Claudia; Ceci, Angelo; Gemkow, Mark J; Nagaraja, Nelamangala V; Romig, Helmut; Sauer, Achim; Riether, Doris.
Afiliación
  • Bartolozzi A; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Cirillo PF; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Berry AK; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Hickey ER; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Thomson DS; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Wu L; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Zindell R; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Albrecht C; Evotec AG, Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
  • Ceci A; Boehringer Ingelheim Pharma GmbH&Co. KG, Birkendorfer Strasse 65, 88397 Biberach an der Riß, Germany.
  • Gemkow MJ; Evotec AG, Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
  • Nagaraja NV; Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
  • Romig H; Boehringer Ingelheim Pharma GmbH&Co. KG, Birkendorfer Strasse 65, 88397 Biberach an der Riß, Germany.
  • Sauer A; Boehringer Ingelheim Pharma GmbH&Co. KG, Birkendorfer Strasse 65, 88397 Biberach an der Riß, Germany.
  • Riether D; Boehringer Ingelheim Pharma GmbH&Co. KG, Birkendorfer Strasse 65, 88397 Biberach an der Riß, Germany.
Bioorg Med Chem Lett ; 25(3): 587-92, 2015 Feb 01.
Article en En | MEDLINE | ID: mdl-25575658
A novel class of potent cannabinoid receptor 2 (CB2) agonists based on a (S)-piperidine scaffold was identified using ligand-based pharmacophore models. Optimization of solubility and metabolic stability led to the identification of several potent CB2 agonists (e.g., 30) that displayed selectivity over cannabinoid receptor 1 (CB1) and acceptable drug like properties. In rats, compound 30 demonstrated a favorable pharmacokinetic profile and efficacy in a Streptozotocin-induced diabetic neuropathy model, with full reversal of mechanical hyperalgesia.
Asunto(s)
Palabras clave
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácidos Pipecólicos / Piperidinas / Tiazinas / Receptor Cannabinoide CB2 Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácidos Pipecólicos / Piperidinas / Tiazinas / Receptor Cannabinoide CB2 Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido