Glutamate (Metabotropic) Receptors

Metabotropic glutamate receptors (mGlus) are coupled to a variety of second messenger systems via G proteins. To date, eight different mGlu subtypes (mGlu1-8) have been cloned and subsequently expressed in various cell lines. These receptors have been classified into 3 groups based on amino acid sequence similarity, agonist pharmacology and the signal transduction pathways to which they couple.

Glutamate (Metabotropic) Receptor Target Files

Related Categories

Group I mGlu receptors (mGlu1 and mGlu5) stimulate inositol phosphate metabolism and mobilization of intracellular Ca2+, whereas group II (mGlu2 and mGlu3) and group III (mGlu4 and mGlu6-8) couple to adenylyl cyclase. In addition to the above groups, a fourth (as yet unassigned) group of metabotropic glutamate receptors which couple to phospholipase D has been reported.

Receptor Subtype Group I Group II Group III PLD Coupled mGlu Receptor
Subtypes mGlu1
mGlu5
mGlu2
mGlu3
mGlu4
mGlu6
mGlu7
mGlu8
Undetermined
Transduction Mechanism ↑ PLC ↓ AC ↓ AC ↑ PLD
Example Agonists L-Quisqualic acid (0188)
(S)-3,5-DHPG (0805)
CHPG (1049)
DCG-IV (0975)
L-CCG-I (0333)
(2R,4S)-APDC (1208)
LY 379268 (2453)
LY 354740 (3246)
L-AP4 (0103)
(S-3,4-DCPG (1302)
ACPT I (1111)
(RS)-PPG (1220)
VU 0155041 (3248)
L-CSA (0216)
Example Antagonists CPCCOEt (1028)
AIDA (0904)
Fenobam (2386)
MPEP (1212)
LY 367385 (1237)
YM 298198 (2448)
(RS)-APICA (1073)
EGLU (0971)
LY 341495 (1209)
CPPG (0972)
MAP4 (0711)
MSOP (0803)
UBP 1112 (1369)
MMPIP (2963)
(RS)-3,5-DHPG (0342)

Properties of Selected Metabotropic Glutamate Receptor Antagonists

Group I

Antagonist mGlu1a mGlu5a mGlu2 mGlu3 mGlu4 mGlu6 mGlu7 mGlu8
(S)-MCPG (0337) 124-543 (Kb) 154-460 (Kb)
> 2000 (Kb)
15 (Ki) 317 (Ki) > 1000 (IC50) > 100 (IC50) > 1000 (IC50) 320 (IC50)
(S)-4CPG (0323) 15-182 (Kb) > 1000 (Kb)
145 (Kb)
> 300 (Kb)
366 (Ki)
Weak agonist
ND > 1000 (IC50) Weak agonist ND Agonist
(S)-4C3HPG (0320) 11.5-393 (Kb) 157 (Kb)
Agonist ND > 1000 (IC50) ND ND Agonist
AIDA (0904) 3.4 (pKb) > 1000 (IC50) Weak agonist ND > 1000 (IC50) ND ND ND
CPCCOEt (1028) 4.76 (pKb) > 100 (IC50) > 100 (IC50) ND > 100 (IC50) ND > 100 (IC50) > 100 (IC50)
MPEP (1212) > 100 (IC50) 0.032 (IC50) > 100 (IC50) ND > 100 (IC50) > 100 (IC50) > 100 (IC50) ND
SIB 1757 (1215) > 1000 (IC50) 0.4 (IC50 > 30 (IC50) ND > 30 (IC50) > 30 (IC50) > 30 (IC50) > 30 (IC50)
SIB 1893 (1214) > 30 (IC50) 0.3 (IC50) > 30 (IC50) ND > 30 (IC50) > 30 (IC50) > 30 (IC50) > 30 (IC50)
LY 367385 (1237) 8.8 (IC50) > 100 (IC50) ND ND ND ND ND ND
3-MATIDA (2196) 6.3 (IC50) > 300 (IC50) > 300 (IC50) ND > 300 (IC50) ND ND ND

Group II and III

Antagonist mGlu1a mGlu5a mGlu2 mGlu3 mGlu4 mGlu6 mGlu7 mGlu8
MPPG (0853) 1100 (IC50) No effect 12 (Ki) ND 22 (KD) 138 (Kb) ND 20 (IC50)
MAP4 (0711) No effect ND 15 (Ki)
Weak agonist
ND 36 (KD)
190 (Ki)
Weak moderate agonist ND 25 (IC50)
DCG IV (0975) 389 (IC50) 630 (IC50)
Agonist Agonist 22.5 (IC50) 39.6 (IC50) 40.1 (IC50) 32 (IC50)
ACPT-II (1112) 115 (Kb) ND 88 (Kb) ND 77 (Kb) ND ND 123 (IC50)
LY 341495 (1209) 6.8 (IC50) 8.2 (IC50) 0.002 (Ki) 0.001 (Ki) 22 (IC50) ND 0.99 (IC50) 0.173 (IC50)

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