Glutamate (Metabotropic) Group I Receptors

Metabotropic glutamate (mGlu) group I receptors are members of the metabotropic class of glutamate receptors, which also includes mGlu group II and mGlu group III receptors. mGlu group I receptors are divided into two subtypes, mGlu1 and mGlu5.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0284 (1S,3R)-ACPD
Group I/group II mGlu agonist
0187 (±)-trans-ACPD
Group I/group II mGlu agonist
1049 CHPG
mGlu5 selective agonist
3695 CHPG Sodium salt
Selective mGlu5 agonist. Sodium salt of CHPG (Cat. No. 1049)
0342 (RS)-3,5-DHPG
Selective group I mGlu agonist
0805 (S)-3,5-DHPG
Selective group I mGlu agonist. Active enantiomer of 3,5-DHPG (Cat. No. 0342)
0324 (RS)-3-Hydroxyphenylglycine
Group I mGlu agonist
0326 (S)-3-Hydroxyphenylglycine
Group I mGlu agonist, active isomer
3331 NPEC-caged-(1S,3R)-ACPD
Caged (1S,3R)-ACPD
0188 L-Quisqualic acid
Very potent group I mGlu agonist
0162 S-Sulfo-L-cysteine sodium salt
Group I agonist

Antagonists

Cat No Product Name / Activity
5229 ABP 688
High affinity human mGlu5 receptor antagonist
2254 ACDPP hydrochloride
Selective mGlu5 receptor antagonist
0904 AIDA
Potent, selective group I mGlu antagonist
0125 DL-AP3
Group I mGlu antagonist
5614 AZD 2066
mGlu5 antagonist; orally bioavailable and brain penetrant
5613 AZD 9272
Potent and selective mGlu5 antagonist; brain penetrant
2501 Bay 36-7620
Non-competitive mGlu1 antagonist with inverse agonist activity
0329 (S)-3-Carboxy-4-hydroxyphenylglycine
Group I antagonist/group II agonist
0320 (S)-4-Carboxy-3-hydroxyphenylglycine
Group I antagonist/group II agonist
0323 (S)-4-Carboxyphenylglycine
Competitive group I mGlu antagonist/weak group II agonist
1028 CPCCOEt
Selective non-competitive mGlu1 receptor antagonist
1009 E4CPG
Group I/group II mGlu antagonist
2386 Fenobam
Potent and selective mGlu5 antagonist
1749 HexylHIBO
Group I mGlu antagonist
1750 (S)-HexylHIBO
Group I mGlu antagonist
2333 JNJ 16259685
Extremely potent, mGlu1-selective non-competitive antagonist
1237 LY 367385
Selective mGlu1a antagonist
2390 LY 456236 hydrochloride
Selective mGlu1 antagonist
2196 3-MATIDA
Potent, selective mGlu1 antagonist
0336 (RS)-MCPG
Non-selective mGlu antagonist
3696 (RS)-MCPG disodium salt
Sodium salt of (RS)-MCPG (Cat. No. 0336)
0337 (S)-MCPG
Non-selective mGlu antagonist. Active isomer of Cat. No. 0336
1212 MPEP hydrochloride
mGlu5 antagonist and positive allosteric modulator at mGlu4
2921 MTEP hydrochloride
Potent, selective mGlu5 antagonist
4134 NPS 2390
Group I mGlu antagonist
1027 PHCCC
Potent group I mGlu antagonist
1215 SIB 1757
Highly selective mGlu5 antagonist
1214 SIB 1893
mGlu5 antagonist and positive allosteric modulator at mGlu4
3413 YM 202074
High affinity, selective mGlu1 antagonist
2986 YM 230888
Selective mGlu1 antagonist
2448 YM 298198 hydrochloride
Highly potent, selective non-competitive mGlu1 antagonist
2447 Desmethyl-YM 298198
Derivative of mGlu1 antagonist YM 298198 (Cat. No. 2448)

Modulators

Cat No Product Name / Activity
4416 ADX 10059 hydrochloride
Negative allosteric modulator at mGlu5
3235 CDPPB
Positive allosteric modulator at mGlu5
4787 CPPHA
Positive allosteric modulator at mGlu1 and mGlu5
1952 DCB
Allosteric modulator at mGlu5
1625 DFB
Allosteric potentiator at mGlu5
1953 DMeOB
Negative allosteric modulator at mGlu5
5000 FTIDC
Potent and selective negative allosteric modulator at mGlu1; also mGlu1 inverse agonist
5275 LSN 2463359
Potent and selective positive allosteric modulator at mGlu5
4438 MFZ 10-7
Negative allosteric modulator at mGlu5
4348 Ro 01-6128
Positive allosteric modulator of mGlu1
4347 Ro 67-4853
Positive allosteric modulator of group I mGlu receptors
4346 Ro 67-7476
Positive allosteric modulator of mGlu1
4381 VU 0285683
Negative allosteric modulator at mGlu5
4437 VU 0357121
Positive allosteric modulator of mGlu5
4323 VU 0360172 hydrochloride
Positive allosteric modulator at mGlu5
4394 VU 0360223
Negative allosteric modulator at mGlu5
5322 VU 0409106
Potent and selective negative allosteric modulator at mGlu5
5693 VU 0409551
Selective mGlu5 positive allosteric modulator; brain penetrant and orally bioavailable
5379 VU 0469650 hydrochloride
Potent and selective negative allosteric modulator of mGlu1
5377 VU 0483605
Positive allosteric modulator at mGlu1
3325 VU 1545
mGlu5 positive allosteric modulator
4458 VU 29
Potent mGlu5 allosteric potentiator

Ligand-sets

Cat No Product Name / Activity
1826 Group I mGlu Receptor Tocriset™
Selection of 5 group I mGlu receptor ligands (Cat. Nos. 0805, 0188, 1237, 1212 and 0337)
1829 Mixed mGlu Receptor Tocriset™
Selection of 5 mixed mGlu receptor ligands (Cat. Nos. 0805, 0975, 0103, 0337 and 1209)

Metabotropic glutamate (mGlu) group I receptors are members of the metabotropic class of glutamate receptors, which also includes mGlu group II and mGlu group III receptors. mGlu group I receptors are divided into two subtypes, mGlu1 and mGlu5. Group I mGluRs are coupled to Gq/11, which activates phospholipase C. They are also associated with Na+ and K+ channels. Their action is generally excitatory, increasing conductance, causing more glutamate to be released from the presynaptic cell. They can also increase inhibitory postsynaptic potentials (IPSPs), inhibit glutamate release and modulate voltage-dependent calcium channels. Group I mGluRs, unlike other groups, are activated by 3,5-dihydroxyphenylglycine (DHPG), allowing their function to be isolated. The human genes for mGluR1 and mGluR5 receptors have been localized to chromosomes 6 (6q24) and 11 (11q14.3) respectively.

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

Literature for Glutamate (Metabotropic) Group I 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 I Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
mGlu1 Human GRM1 NM_000838 Q13255
Mouse Grm1 NM_001114333 P97772
Rat Grm1 NM_017011 P23385
mGlu5 Human GRM5 NM_000842 P41594
Mouse Grm5 NM_001081414 Q3UVX5
Rat Grm5 NM_017012 P31424