Abcam Biochemicals (formerly Ascent Scientific)

mGlu Product Range

mGlu Group I
Group I and Group II
Group II
Group III

mGlu receptors - @ a glance

Metabotropic glutamate (mGlu) receptors are activated by the neurotransmitter L-glutamate. The receptors are classified into 3 groups based on agonist pharmacology, primary amino acid sequence and signal transduction mechanism. In addition to ligands that act directly at the orthosteric glutamate recognition site, negative and positive allosteric modulators (NAMs and PAMs) and allosteric agonists have been described. PAMs typically potentiate an orthosteric agonist response, but have no significant agonist action alone, whereas allosteric agonists do not bind to the orthosteric site but can activate G-protein coupling in the absence of an orthosteric agonist.

mGlu receptor ligands - subunit selectivity

Receptor group
Group I 
 Group I
 Group II
Group II 
Receptor subtype mGlu1 mGlu5 mGlu2 mGlu3
Other names mGluR1 mGluR5 mGluR2 mGluR3
Principal transduction Gq/11 Gq/11 Gi/o Gi/o
Example agonists (S)-3,5-DHPG (R,S)-CHPG
(S)-3,5-DHPG
LY 354740
LY 379268
LY 354740
LY 379268
Example positive allosteric modulators Ro01-6128
Ro67-4853
Ro67-7476
DFB
CPPHA
CDPPB
LY487379
CBiPES
Example competitive antagonists LY 341495 (micromolar)
LY367385
LY 341495 (micromolar) LY 341495 (low nanomolar) LY 341495 (low nanomolar)
Example negative allosteric modulators CPCCOEt
LY456236
YM298198
MPEP
MTEP
fenobam
Receptor group
Group III 
 Group III
Group III 
Group III
Receptor subtype mGlu4 mGlu6 mGlu7 mGlu8
Other names mGluR4 mGluR6 mGluR7 mGluR8
Principal transduction Gi/o Gi/o Gi/o Gi/o
Example agonists L-AP4 L-AP4 L-AP4
AMN082 (allosteric agonist)
L-AP4
(S)-3,4-DCPG
Example positive allosteric modulators VU0155041
PHCCC
Example competitive antagonists LY 341495 (micromolar) LY 341495 (micromolar) LY 341495 (micromolar) LY 341495 (high nanomolar)
Example negative allosteric modulators MMPIP

Receptor group
mGlu1a
mGlu5a mGlu2 mGlu3 mGlu4
mGlu6
mGlu7
mGlu8
LY 341495 6.8 (IC50)1 8.2 (IC50)1 0.002 (Ki)2 0.001 (Ki)2 22 (IC50)1 ND 0.99 (IC50)1 0.173 (IC50)1
YM298198 0.016 (IC50)3 >10 (IC50)3 >10 (IC50)3 >10 (IC50)3 >10 (IC50)3 >10 (IC50)3 >10 (IC50)3 _
(S)-MCPG 124-543 (Kb)4,5 154-460 (Kb)4,6
>2000 (Kb)5
15 (Ki)7 317 (Ki)8 >1000 (IC50)9 >100 (IC50)10 >1000 (IC50)11 320 (IC50)12
CPCCOEt 4.76 (pKb)13 >100 (IC50)14 >100 (IC50)14 ND >100 (IC50)14 ND >100 (IC50)14 >100 (IC50)14
MPEP >100 (IC50)15 0.032 (IC50)15 >100 (IC50)15 ND >100 (IC50)15 >100 (IC50)15 >100 (IC50)15 ND
LY367385 8.8 (IC50)2 >100 (IC50)2 ND ND ND ND ND ND
MMPIP >116 >116 >116 >116 >116 ND 0.026 >1

References

  1. Kingston et al (1995) Neuropharmacology 34:887
  2. Johnson et al (1999) Neuropharmacology 38:1519
  3. Kohara et al (2005) JPET. 315:163
  4. Lin et al (1997) Neuropharmacology 36: 917
  5. Brabet et al (1995) Neuropharmacology. 34:895
  6. Doherty et al (1999) Br J Pharmacol 126:205
  7. Cartmell et al (1998) Br j Pharmacol 123: 497
  8. Laurie et al (1995) Naunyn-SchmiedArch.Pharmacol. 351:565
  9. Hayashi et al (1994) J Neurosci 14:3370
  10. Laurie et al (1997) Neuropharmacology 36:145
  11. Saugstad et al (1994) Mol.Pharmacol. 45:367
  12. Saugstad et al (1997) Mol. Pharmacol. 51:119
  13. Hermans et al (1998) Br J Pharmacol 126 873
  14. Litschig et al (1999) Mol Pharmacol. 55:453
  15. Neuropharmacology38: 1493
  16. Suzuki et al (2007) J Pharmacol Exp Ther. 323:147

mGlu receptor resources

For further information please see:

Glutamate receptors - @ a glance
Guide to Receptors and Channels (GRAC), British Journal of Pharmacology
IUPHAR-DB

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