447459-97-4Relevant academic research and scientific papers
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies
Shankar, Bandarpalle B.,Lavey, Brian J.,Zhou, Guowei,Spitler, James A.,Tong, Ling,Rizvi, Razia,Yang, De-Yi,Wolin, Ronald,Kozlowski, Joseph A.,Shih, Neng-Yang,Wu, Jie,Hipkin, R. William,Gonsiorek, Waldemar,Lunn, Charles A.
, p. 4417 - 4420 (2007/10/03)
We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as th
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: Identification of a lead and initial SAR studies
Lavey, Brian J.,Kozlowski, Joseph A.,Hipkin, R. William,Gonsiorek, Waldemar,Lundell, Daniel J.,Piwinski, John J.,Narula, Satwant,Lunn, Charles A.
, p. 783 - 786 (2007/10/03)
A novel class of cannabinoid CB2 receptor ligands is described. These triaryl bis-sulfones are nanomolar inhibitors of the CB2 receptor and show high selectivity over the cannabinoid CB1 receptor. One example of this new class decreases ligand-induced GTPγS binding to recombinant CB2 cell membranes, identifying the compound as a CB2-selective inverse agonist.
Cannabinoid receptor ligands
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Page 32, (2008/06/13)
The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmac
Substituted 2-(R)-Methyl piperazines as muscarinic M2 selective ligands
Kozlowski, Joseph A,Zhou, Guowei,Tagat, Jayaram R.,Lin, Sue-Ing,McCombie, Stuart W.,Ruperto, Vilma B.,Duffy, Ruth A.,McQuade, Robert A.,Crosby Jr., Gordon,Taylor, Lisa A.,Billard, William,Binch III, Herbert,Lachowicz, Jean E.
, p. 791 - 794 (2007/10/03)
A novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described. They are potent M2 selective ligands that have > 100-fold selectivity versus the M1 receptor. In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration.
