Glutamate (Metabotropic) Group III Receptors

Metabotropic Glutamate (mGlu) group III receptors are members of the metabotropic class of glutamate receptors, which also includes mGlu group I and mGlu group II receptors. Group III receptors are divided into four subtypes, mGlu4, mGlu6, mGlu7 and mGlu8.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1111 ACPT-I
Group III mGlu agonist
2385 AMN 082 dihydrochloride
The first selective mGlu7 agonist
0103 L-AP4
Selective group III mGlu agonist
4119 Cinnabarinic acid
Selective mGlu4 agonist
1394 (RS)-3,4-DCPG
Potent systemically active anticonvulsant. Racemate of (S)-3,4-DCPG (Cat. No. 1302)
1302 (S)-3,4-DCPG
Potent, selective mGlu8a agonist
3330 NPEC-caged-(S)-3,4-DCPG
Caged (S)-3,4-DCPG
0238 O-Phospho-L-serine
Group III mGlu agonist
1220 (RS)-PPG
Potent, selective mGlu8 agonist
3248 VU 0155041
Potent, positive allosteric mGlu4 agonist
3311 VU 0155041 sodium salt
Potent, positive allosteric mGlu4 agonist. Sodium salt of VU 0155041 (Cat. No. 3248)
3249 Z-Cyclopentyl-AP4
Group III mGlu agonist (mGlu4 > mGlu8 > mGlu7)

Antagonists

Cat No Product Name / Activity
0972 CPPG
Potent group III mGlu antagonist
1209 LY 341495
Group II/III antagonist
4062 LY 341495 disodium salt
Disodium salt of LY 341495 (Cat. No. 1209)
0711 MAP4
Selective group III mGlu antagonist. Also potent group II/group III mGlu agonist
2963 MMPIP hydrochloride
Potent, allosteric mGlu7-selective antagonist
0853 MPPG
Group III/group II mGlu antagonist. More selective for group III than group II
0803 MSOP
Specific group III mGlu antagonist
0854 MSPG
Group III/group II mGlu antagonist
1369 UBP1112
Group III mGlu antagonist
5248 XAP 044
Potent and selective mGlu7 antagonist

Modulators

Cat No Product Name / Activity
5715 (±)-ADX 71743
Negative allosteric modulator at mGlu7; brain penetrant
4832 AZ 12216052
Positive allosteric modulator at mGlu8
1212 MPEP hydrochloride
Positive allosteric modulator at mGlu4 and mGlu5 antagonist
1214 SIB 1893
Positive allosteric modulator at mGlu4 and mGlu5 antagonist
4370 TC-N 22A
Potent, selective mGlu4 positive allosteric modulator
4259 TCN 238
Positive allosteric modulator of mGlu4
3707 VU 0361737
Selective positive allosteric modulator at mGlu4
4371 VU 0364439
Positive allosteric modulator at mGlu4
4469 VU 0364770
Positive allosteric modulator at mGlu4
5378 VU 0422288
Selective group III mGlu positive allosteric modulator

Ligand-sets

Cat No Product Name / Activity
1828 Group III mGlu Receptor Tocriset™
Selection of 5 group III mGlu receptor ligands (Cat. Nos. 0103, 1220, 0972, 0803 and 1209)
1829 Mixed mGlu Receptor Tocriset™
Selection of 5 mixed mGlu receptor ligands (Cat. Nos. 0805, 0975, 0103, 0337 and 1209)

Other

Cat No Product Name / Activity
4936 Clozapine N-oxide
Activator of muscarinic DREAADs

Metabotropic Glutamate (mGlu) group III receptors are members of the metabotropic class of glutamate receptors, which also includes mGlu group I and mGlu group II receptors. Group III receptors are divided into four subtypes, mGlu4, mGlu6, mGlu7 and mGlu8. mGlu group III receptors are coupled to Gi/o, which inhibits adenylyl cyclase, decreasing the formation of cAMP. These receptors are involved in spatial learning and memory, and umami taste (mGlu4), stimulation of photoreceptors (mGlu6), long term depression (mGlu7) and presynaptic inhibition in the perforant pathway (mGlu8). The human genes for mGlu4, mGlu6, mGlu7 and mGlu8 receptors have been localized to chromosomes 6 (6p21.3), 5 (5q35), 3 (3p26-p25) and 7 (7q31.3-q32.1) respectively.

External sources of pharmacological information for Glutamate (Metabotropic) Group III Receptors :

Literature for Glutamate (Metabotropic) Group III Receptors

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Metabotropic Glutamate Receptors

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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Glutamate (Metabotropic) Group III Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
mGlu4 Human GRM4 NM_000841 Q14833
Mouse Grm4 NM_001013385 Q68EF4
Rat Grm4 NM_022666 P31423
mGlu6 Human GRM6 NM_000843 O15303
Mouse Grm6 BC034118 Q5NCH9
Rat Grm6 NM_022920 P35349
mGlu7 Human GRM7 NM_000844 Q14831
Mouse Grm7 NM_177328 Q68ED2
Rat Grm7 NM_031040 P35400
mGlu8 Human GRM8 NM_000845 O00222
Mouse Grm8 NM_008174 P47743
Rat Grm8 NM_022202 P70579