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Synthesis and pharmacological characterisation of subtype selective group III metabotropic glutamate receptor agonists

Reference	B14707
Principal Investigator / Supervisor	Professor David Jane
Co-Investigators / Co-Supervisors
Institution	University of Bristol
Department	Physiology and Pharmacology
Funding type	Research
Value (£)	97,934
Status	Completed
Type	Research Grant
Start date	12/03/2001
End date	12/03/2003
Duration	24 months

Abstract

Agonists for individual subtypes of group III mGlu receptors are currently unavailable. We have recently identified DCPG to be a potent and selective mGlu8 receptor agonist. We aim to further increase the potency and bioavailability of DCPG by synthesising novel analogues. These will be tested on mGlu 4, 6, 7 and 8 receptors in order to determine their selectivity and using this and previous data, pharmacophore models will be constructed for each receptor subtype. Radioligands will also be synthesised allowing binding assays to be set up for native group III mGluRs. In addition, selective agonists will be used by pharmacologists within the group and by our collaborators to assess the physiological roles of mGlu4, 6, 7 and 8 receptors.

Summary

unavailable

Committee	Closed Committee - Biomolecular Sciences (BMS)
Research Topics	X – not assigned to a current Research Topic
Research Priority	X – Research Priority information not available
Research Initiative	X - not in an Initiative
Funding Scheme	X – not Funded via a specific Funding Scheme

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