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Dressman, Bruce A.; Tromiczak, Eric G.; Chappell, Mark D.; Tripp, Allie E.; Quimby, Steven J.; Vetman, Tatiana; Fivush, Adam M.; Matt, James; Jaramillo, Carlos; Li, Renhua; Khilevich, Albert; Blanco, Maria-Jesus; Smith, Stephon C.; Carpintero, Mercedes; de Diego, José Eugenio; Barberis, Mario; García-Cerrada, Susana; Soriano, José F.; Schkeryantz, Jeffrey M.; Witkin, Jeffrey M.; Wafford, Keith A.; Seidel, Wesley; Britton, Thomas; Overshiner, Carl D.; Li, Xia; Wang, Xu-Shan; Heinz, Beverly A.; Catlow, John T.; Swanson, Steven; Bedwell, David; Ornstein, Paul L.; Mitch, Charles H.
Bioorganic & medicinal chemistry letters, 12/2016, Letnik: 26, Številka: 23Journal Article
Display omitted Negative modulators of metabotropic glutamate 2 & 3 receptors demonstrate antidepressant-like activity in animal models and hold promise as novel therapeutic agents for the treatment of major depressive disorder. Herein we describe our efforts to prepare and optimize a series of conformationally constrained 3,4-disubstituted bicyclo3.1.0hexane glutamic acid analogs as orthosteric (glutamate site) mGlu2/3 receptor antagonists. This work led to the discovery of a highly potent and efficacious tool compound 18 (hmGlu2 IC50 46±14.2nM, hmGlu3 IC50=46.1±36.2nM). Compound 18 showed activity in the mouse forced swim test with a minimal effective dose (MED) of 1mg/kg ip. While in rat EEG studies it exhibited wake promoting effects at 3 and 10mg/kg ip without any significant effects on locomotor activity. Compound 18 thus represents a novel tool molecule for studying the impact of blocking mGlu2/3 receptors both in vitro and in vivo.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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in: SICRIS
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