In the original article, there was a mistake in Figure 1 as published. The chirality of L-AP4 and LSP1-2111 was incorrect. pEC50 values have also been corrected for LSP1-2111 in Table 1. The authors apologize for these errors and state that they do not change the scientific conclusions of the article in any way. The original article has been updated.
Figure 1.
Current tool compounds used to study mGlu7.
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) | Orthosteric agonist | 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., 2014 |
| 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 parentheses: PIH, Phosphatidylinositol hydrolysis; cAMP, cAMP accumulation; Ca2+, Calcium mobilization; GTPγS, GTPγS binding.
Conflict of Interest Statement
The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
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