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Agonists of cyclic AMP-coupled metabotropic glutamate receptors in adult rat cortical slices

European Journal of Pharmacology, ISSN: 0014-2999, Vol: 309, Issue: 1, Page: 79-85
1996
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Article Description

A number of potential Group 2 and Group 3 metabotropic glutamate receptor (mGlu receptor) agonists were investigated in adult rat brain cerebrocortical slices. The rank order of their potency in inhibiting forskolin-stimulated adenylyl cyclase was found to be: ( S )-2-amino-2-methyl-4-phosphonobutyric acid (MAP4) > (2 S,1′ S,2′ S )-2-(2-carboxycyclopropyl)glycine ( l -CCG-I) > (1 S,3 S )-1-aminocyclopentane-1,3-dicarboxylic acid (1 S,3 S -ACPD) > (1 S,3 R )-1-aminocyclopentane-1,3-dicarboxylic acid (1 S,3 R )-ACPD) > (2 S,1′ R,2′ R,3′ R )-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) > ( S )-2-methylglutamate (( S )-MG) > l -glutamate > (2 S,1′ S,2′ S )-2-(2-carboxycyclopropyl)alanine ((MCCG) > l -2-amino-4-phosphonobutyric acid ( l -AP4) > l -serine- O -phosphate (SOP). The finding that ( S )-2-amino-2-methyl-4-phosphonobutyric acid was the most potent agonist at these metabotropic glutamate receptors is in contrast to its observed potent mGlu receptor antagonist action in the neonatal rat spinal cord.

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