Synthesis and pharmacological characterisation of 2,4-Dicarboxy-pyrroles as selective non-Competitive mGluR1 antagonists
2003
Abstract Metabotropic glutamate receptors (mGluRs) are an unusual family of G-protein coupled receptor (GPCR), and are characterised by a large extracellular N-terminal domain that contains the glutamate binding site. We have identified a new class of non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonists, 2,4-dicarboxy-pyrroles which are endowed with nanomolar potency. They interact within the 7 transmembrane (7TM) domain of the receptor and show antinociceptive properties when tested in a number of different animal models.
Keywords:
- Metabotropic glutamate receptor 7
- Organic chemistry
- Metabotropic glutamate receptor 4
- Metabotropic glutamate receptor 3
- Metabotropic glutamate receptor 2
- Metabotropic glutamate receptor
- Metabotropic glutamate receptor 6
- Metabotropic glutamate receptor 5
- Biochemistry
- Metabotropic glutamate receptor 1
- Stereochemistry
- Chemistry
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