Table 1.
Summary of current tool compounds used to study mGlu7.
| Name (#) | Type | mGlu7 pEC50/pIC50 | mGlu8 pEC50/pIC50 | mGlu4 pEC50/pIC50 | mGlu6 pEC50/pIC50 | Source |
|---|---|---|---|---|---|---|
| L-AP4 (1) | Orthosteric agonist | 3.47 (PIH) | 6.53 (PIH) | 7.00 (PIH) | 5.62 (PIH) | Acher et al., 2012; Selvam et al., 2018 |
| 3.61 (Ca2+) | 6.53 (Ca2+) | 6.89 (Ca2+) | 6.00 (Ca2+) | |||
| LSP4-2022 (2) | Orthosteric agonist | 4.34 (Ca2+) | 4.54 (Ca2+) | 6.96 (Ca2+) | 5.36 (Ca2+) | Acher et al., 2012; Goudet et al., 2012; Selvam et al., 2018 |
| LSP1-2111 (3) | Orthosteric agonist | 4.28 (PIH) | 4.18 (PIH) | 5.66 (PIH) | 5.77 (PIH) | Selvam et al., 2018 |
| 4.00 (Ca2+) | 4.71 (Ca2+) | 6.05 (Ca2+) | 5.49 (Ca2+) | |||
| LSP2-9166 (4) | 5.71 (Ca2+) | 4.25 (Ca2+) | 7.22 (Ca2+) | Not reported | Acher et al., 2012 | |
| VU0422288 (5) | Group III PAM | 6.85 (Ca2+) | 6.93 (Ca2+) | 6.98 (Ca2+) | Not reported | Jalan-Sakrikar et al., 2014 |
| VU0155094 (6) | Group III PAM | 5.80 (Ca2+) | 6.07 (Ca2+) | 5.48 (Ca2+) | Not reported | Jalan-Sakrikar et al., 2014 |
| ADX88178 (7) | mGlu4/8 PAM | >4.52 (Ca2+) | 5.66 (Ca2+) | 8.46 (Ca2+) | >5 | Le Poul et al., 2012 |
| ADX71743 (8) | mGlu7 NAM | 7.20 (human, Ca2+) | Inactive | Inactive | Inactive | Kalinichev et al., 2013 |
| 7.06 (rat, Ca2+) | Inactive | Inactive | Inactive | |||
| AMN082 (9) | Allosteric agonist | 6.59 (GTPγS) | >5 (GTPγS) | >5 (GTPγS) | >5 (GTPγS) | Mitsukawa et al., 2005 |
| XAP044 (10) | Antagonist | 5.26 (cAMP) | 4.48 (cAMP) | Inactive | Inactive | Gee et al., 2014 |
| 5.55 to 5.46 (GTPγS) | ||||||
| LY341495 (11) | Orthosteric antagonist | 6.00 (cAMP) | 6.76 (cAMP) | 4.66 (cAMP) | Not reported | Kingston et al., 1998 |
| MMPIP (12) | mGlu7 NAM | 6.66 (cAMP) | >5 (cAMP) | >5 (cAMP) | Not reported | Suzuki et al., 2007 |
| 7.15 (Ca2+) | Niswender et al., 2010 | |||||
| 6.14 (Thallium) | Niswender et al., 2010 | |||||
| VU6010608 (13) | mGlu7 NAM | 6.12 (Ca2+) | >5 (Ca2+) | >5 (Ca2+) | Inactive (>5) | Reed et al., 2017 |
| VU6005649 (14) | mGlu7/8 PAM | 6.19 (Ca2+) | 5.59 (Ca2+) | >5 (Ca2+) | Inactive | Abe et al., 2017 |
NAM, negative allosteric modulator; PAM, positive allosteric modulator; EC50, effective concentration 50; IC50, inhibitory concentration 50. Assay type is indicated in parenthesis: PIH, phosphatidylinositol hydrolysis; cAMP, cAMP accumulation; Ca2+, calcium mobilization; GTPγS, GTPγS binding.