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.
MeSH terms
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Administration, Oral
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Animals
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Cyclic AMP / biosynthesis
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Fear
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Glycine / analogs & derivatives
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Glycine / chemical synthesis*
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Glycine / chemistry
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Glycine / pharmacology
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In Vitro Techniques
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Male
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Motor Activity / drug effects
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Rats
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Rats, Sprague-Dawley
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Receptors, Metabotropic Glutamate / agonists*
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Reflex, Startle / drug effects
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Stereoisomerism
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Structure-Activity Relationship
Substances
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2-(2'-carboxy-3'-hydroxymethylcyclopropyl)glycine
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2
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metabotropic glutamate receptor 3
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Cyclic AMP
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Glycine