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. 2017 Oct 21;174(Suppl Suppl 1):S17–S129. doi: 10.1111/bph.13878
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]