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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) tADA (0860) 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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