I: CPCCOEt | | IC50 = 6.5 μM | First allosteric mGlu receptor modulator | Annoura et al., 1996; Hermans et al., 1998; Litschig et al., 1999 |
II: BAY36-7620 | | IC50 = 160 nM | Inverse allosteric agonist | Carroll et al., 2001 |
III: A841720 | | IC50 = 11 nM | Analgesic activity and disruption of cognitive function in rats in vivo | El-Kouhen et al., 2006 |
IV: JNJ16259685 | | IC50 = 3.2 nM | High occupancy of mGlu1 receptors in rat brain after systemic application | Lavreysen et al., 2004 |
V: YM-298198 | | IC50 = 16 nM | Analgesic activity in mice after oral application | Kohara et al., 2005 |
VI: EM-TBPC | | IC50 = 15 nM KD = 6.6 nM | Used as a radioligand in its tritiated form for mapping studies; has high affinity for rat but not for human receptor | Malherbe et al., 2003 |
VII: CFMMC | | IC50 = 50 nM | | Fukuda et al., 2009 |
VIII: FTIDC | | IC50 = 6 nM | Active in formalin pain model | Suzuki et al., 2007a |