(2<i>S</i>,1‘<i>S</i>,2‘<i>R</i>,3‘<i>R</i>)-2-(2‘-Carboxy-3‘-hydroxymethylcyclopropyl) Glycine Is a Highly Potent Group 2 and 3 Metabotropic Glutamate Receptor Agonist with Oral Activity - Concepedia

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(2<i>S</i>,1‘<i>S</i>,2‘<i>R</i>,3‘<i>R</i>)-2-(2‘-Carboxy-3‘-hydroxymethylcyclopropyl) Glycine Is a Highly Potent Group 2 and 3 Metabotropic Glutamate Receptor Agonist with Oral Activity

DOI Full Paper Access

36

Citations

33

References

2003

Year

Iván Collado, Concepción Pedregal, Ana B. Bueno, Alicia Marcos, Rosario González, Jaime Blanco‐Urgoiti, Javier Pérez‐Castells, Darryle D. Schoepp, Rebecca A. Wright, Bryan G. Johnson,

Journal of Medicinal Chemistry

PsychopharmacologyPharmacotherapyMolecular PharmacologyMedicinal ChemistryBiological ActivityBiochemistryPsychiatryPcp-induced Motor ActivationG Protein-coupled ReceptorAsymmetric SynthesisMechanism Of ActionReceptor (Biochemistry)NeuropharmacologyOral ActivityPharmacologyFunctional SelectivityNatural SciencesNeuroscienceBiological PsychiatryMedicineDrug Discovery

Abstract

The asymmetric synthesis and biological activity of (2S,1'S,2'R,3'R)-2-(2'-carboxy-3'-hydroxymethylcyclopropyl) glycine ((+)-3) is described. This novel C-3' substituted carboxy cyclopropyl glycine is a highly potent group 2 and group 3 mGluR agonist that has proven to be orally active in both fear potentiated startle (animal model for anxiety) and PCP-induced motor activation (animal model for psychosis) assays in rats.

References

	Year	Citations

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