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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 3115:163
4. Lin et al (1997) Neuropharmacology 36: 917
5. Brabet et al (1997) Neuropharmacology 36: 917
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 Gasparini et al (1999)
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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