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Chemical Name:N-Phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carbox
amide
Biological Activity:
Group I metabotropic glutamate receptor antagonist (IC50
~ 3 μM); 67 times more potent than
(S)-4-carboxyphenylglycine (Cat. No. 0323). Also a positive allosteric
modulator for mGlu4a; potentiates L-AP4-mediated inhibition
of striatopallidal synaptic transmission in vitro. Displays antiParkinsonian
effects in rats in vivo.
Annouraet
al (1996) A novel class of antagonists for metabotropic glutamate
receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates.
Bioorg.Med.Chem.Lett. 6 763. Maoand Wang (2001)
Selective activation of group I metabotropic glutamate receptors upregulates
preprodynorphin, substance P and preproenkephalin mRNA expression in rat dorsal
striatum. Synapse 39 82.Floret al (2002)
Positive allosteric modulators of metabotropic glutamate receptor subtype 4:
pharmacological and molecular characterization. Neuropharmacology 43
286 Abstr.No. 47. Marinoet al (2003) Allosteric modulation of
group III metabotropic glutamate receptor 4: a potential approach to
Parkinson's disease treatment. Proc.Natl.Acad.Sci.USA 100 13668.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.
