Nomenclature |
mGlu
1 receptor |
mGlu
2 receptor |
mGlu
3 receptor |
mGlu
4 receptor |
mGlu
5 receptor |
HGNC, UniProt |
GRM1, Q13255
|
GRM2, Q14416
|
GRM3, Q14832
|
GRM4, Q14833
|
GRM5, P41594
|
Endogenous agonists |
L‐glutamic acid [1574] |
L‐glutamic acid [1574] |
L‐glutamic acid [1574], NAAG [1750] |
L‐glutamic acid [1574] |
L‐glutamic acid [1574] |
Agonists |
– |
– |
– |
L‐AP4 [2138], L‐serine‐O‐phosphate [2138] |
– |
Selective agonists |
– |
– |
– |
LSP4‐2022 [666] |
(S)‐(+)‐CBPG (Partial agonist) [1261] – Rat, CHPG [1407] |
Antagonists |
LY367385 (pIC50 5.1) [364] |
– |
– |
MAP4 (pK
i 4.6) [721] – Rat |
– |
Selective antagonists |
3‐MATIDA (pIC50 5.2) [1386] – Rat, (S)‐(+)‐CBPG (pIC50 4.2) [1261] – Rat, (S)‐TBPG (pIC50 4.2) [381] – Rat, AIDA (pA2 4.2) [1387] |
PCCG‐4 (pIC50 5.1) [1551] – Rat |
– |
– |
ACDPP (pIC50 6.9) [186] |
Allosteric modulators |
– |
CBiPES (Positive) (pEC50 7) [917], 4‐MPPTS (Positive) (pIC50 5.8) [100, 916, 917, 1731] |
– |
SIB‐1893 (Positive) (pEC50 6.3–6.8) [1281], MPEP (Positive) (pEC50 6.3–6.6) [1281], PHCCC (Positive) (pEC50 4.5) [1247] |
3,3'‐difluorobenzaldazine (Positive) (pIC50 5.6–8.5) [1481, 1482], alloswitch‐1 (Negative) (pIC50 8.1) [1583] – Rat, CDPPB (Positive) (pEC50 7.6–8) [1002, 1180], MTEP (Negative) (pK
i 7.8) [228], MPEP (Negative) (pIC50 7.4–7.7) [609, 611], fenobam (Negative) (pIC50 7.2) [1592], SIB‐1893 (Negative) (pIC50 5.9–6.5) [609, 2028], SIB‐1757 (Negative) (pIC50 6–6.4) [609, 2028], CPPHA (Positive) (pIC50 6.3) [1482] |
Selective allosteric modulators |
BAY 367620 (Negative) (pK
i 9.5) [279] – Rat, JNJ16259685 (Negative) (pIC50 8.9) [1104], Ro01‐6128 (Positive) (pK
i 7.5–7.7) [1019] – Rat, LY456236 (Negative) (pIC50 6.9) [1160], CPCCOEt (Negative) (pIC50 5.2–5.8) [1183] |
Ro64‐5229 (Negative) (pIC50 7) [1031] – Rat, biphenylindanone A (Positive) (pEC50 7) [187] |
– |
VU0361737 (Positive) (pEC50 6.6) [508], VU0155041 (Positive) (pEC50 6.1) [1468] |
VU‐1545 (Positive) (pEC50 8) [429] |