Synthesis and Pharmacological Characterization of C4<sub>ß</sub>-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu<sub>3</sub> Receptor Agonist.

Monn, James A; Henry, Steven S; Massey, Steven M; Clawson, David K; Chen, Qi; Diseroad, Benjamin A; Bhardwaj, Rajni M; Atwell, Shane; Lu, Frances; Wang, Jing; Russell, Marijane; Heinz, Beverly A; Wang, Xu-Shan; Carter, Joan H; Getman, Brian G; Adragni, Kofi; Broad, Lisa M; Sanger, Helene E; Ursu, Daniel; Catlow, John T; Swanson, Steven; Johnson, Bryan G; Shaw, David B; McKinzie, David L; Hao, Junliang

Synthesis and Pharmacological Characterization of C4_ß-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu₃ Receptor Agonist.

Monn, James A; Henry, Steven S; Massey, Steven M; Clawson, David K; Chen, Qi; Diseroad, Benjamin A; Bhardwaj, Rajni M; Atwell, Shane; Lu, Frances; Wang, Jing; Russell, Marijane; Heinz, Beverly A; Wang, Xu-Shan; Carter, Joan H; Getman, Brian G; Adragni, Kofi; Broad, Lisa M; Sanger, Helene E; Ursu, Daniel; Catlow, John T; Swanson, Steven; Johnson, Bryan G; Shaw, David B; McKinzie, David L; Hao, Junliang.

J Med Chem ; 61(6): 2303-2328, 2018 03 22.

Article in En | MEDLINE | ID: mdl-29350927

Subject(s)

Bridged Bicyclo Compounds/chemical synthesis; Bridged Bicyclo Compounds/pharmacology; Excitatory Amino Acid Agonists/chemical synthesis; Excitatory Amino Acid Agonists/pharmacology; Receptors, Metabotropic Glutamate/agonists; Animals; Bridged Bicyclo Compounds/pharmacokinetics; Crystallography, X-Ray; Cyclic AMP/pharmacology; Excitatory Amino Acid Agonists/pharmacokinetics; Excitatory Amino Acid Antagonists/pharmacology; Humans; Male; Models, Molecular; Molecular Docking Simulation; Molecular Structure; Motor Activity/drug effects; Neurons/drug effects; Neurons/metabolism; Phencyclidine/antagonists & inhibitors; Phencyclidine/pharmacology; Protein Binding; Rats; Rats, Sprague-Dawley

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Full text: 1 Database: MEDLINE Main subject: Bridged Bicyclo Compounds / Receptors, Metabotropic Glutamate / Excitatory Amino Acid Agonists Type of study: Diagnostic_studies Limits: Animals / Humans / Male Language: En Year: 2018 Type: Article

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