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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
Nomenclature mGlu1 receptor mGlu5 receptor
HGNC, UniProt GRM1, Q13255 GRM5, P41594
Principal transduction Gq/11 Gq/11
Selective agonists (pKi) (S)-(+)-CBPG (Partial agonist) (pEC50 4.3 - Rat) 1225, CHPG (pIC50 3.4) 1232
Selective antagonists (pKi) AIDA (pA2 4.2) 1231, 3-MATIDA (pIC50 5.2-Rat) 1230, LY367385 (pIC50 5.1) 1196, (S)-(+)-CBPG (pIC50 4.2-Rat) 1225, (S)-TBPG (pIC50 4.2-Rat) 1197 ACDPP (pIC50 6.9) 1188
Selective allosteric regulators PHCCC (Positive), Ro67-7476 (Positive) (pKi 7.5–7.9 - Rat) 1213, Ro01-6128 (Positive) (pKi 7.5–7.7 - Rat) 1213, Ro67-4853 (Positive) (pKi 5.1 - Rat) 1213, JNJ16259685 (Negative) (pIC50 8.9) 1217, A-841720 (Negative) (pIC50 8.0) 1255, 3,5-dimethyl PPP (Negative) (pIC50 7.8-Rat) 1227, YM298198 (Negative) (pIC50 7.8-Rat) 1214, BAY 367620 (Negative) (pIC50 6.8–8.0-Rat) 1193,1216, EM-TBPC (Negative) (pIC50 6.9-Rat) 1223, LY456236 (Negative) (pIC50 6.9) 1218, CPCCOEt (Negative) (pIC50 5.2–5.8) 1220 MTEP (Negative) (pKi 7.8) 1191, VU-1545 (Positive) (pEC50 8.0) 1198, CDPPB (Positive) (pEC50 7.6–8.0) 1211,1219, MPEP (Negative) (pIC50 7.4–7.7) 1202,1204, fenobam (Negative) (pIC50 7.2) 1241, DFB (Positive) (pIC50 5.6–8.5) 1236,1237, CPPHA (Positive) (pIC50 6.3) 1237, SIB-1757 (Negative) (pIC50 6.0–6.4) 1202,1252, SIB-1893 (Negative) (pIC50 5.9–6.5) 1202,1252