Table 1.

Summary of Drugs Targeting Gp1 mGluR-Related Diseases.

Disease	Drugs	Selectivity	Effect	Model	Reference
AD	CTEP	mGluR5 NAM	Prevents cognitive impairment	APP/PS1 mouse	Lindemann and others 2011; Lindemann and others 2015
ASD	JNJ16259685 Fenobam	mGlu1 antagonist mGlu5 antagonist	Recue social interaction and repetitive behaviors	Eif4ebp2 knockout mouse	Aguilar-Valles and others 2015; Modi and others 2018
ASD	CFMTI	mGluR1 antagonist	Improves social interaction	MK-801 rat	Satow and others 2009
Epilepsy	LY367385 AIDA	mGluR1 antagonists	Suppress motor seizures	DBA/2 mouse Lethargic mouse Genetically epilepsy-prone rat	Chapman and others 1999
Epilepsy	MPEP SIB-1893	mGluR5 antagonists	Suppress clonic seizures	DBA/2 mouse Lethargic mouse	Chapman and others 2000
Epilepsy	LY456236	mGluR5 antagonist	Inhibits clonic-tonic seizures Inhibits limbic seizures Decreases behavioral and electrographic seizures Decrease generalized seizures	DBA/2 mouse SD rat	Shannon and others 2005
PD	LY367385 MPEP	mGluR1 antagonist mGluR5 antagonist	Slow degeneration of dopaminergic neurons Prevent striatal dopamine depletion Attenuate parkinsonian motor deficits Decrease dyskinesia	6-OHDA rodent MPTP monkey Parkinsonian rat and monkey	Aguirre and others 2001; Ambrosi and others 2010; Breysse and others 2003; Dekundy and others 2006; Johnston and others 2010; Mela and others 2007; Rylander and others 2010; Vernon and others 2007
PD	MTEP	mGluR5 NAM	Reduces neurodegeneration	MPTP non-human primate	Masilamoni and others 2011
PD	Fenobam	mGluR5 NAM	Reduces dyskinesia	6-OHDA rat MPTP monkey	Ko and others 2014; Rylander and others 2010
PD	Dipraglurant	mGluR5 NAM	Reduces severity of dyskinesia	MPTP macaque PD patient	Bezard and others 2014; Tison and others 2016
PD	AFQ056-mavoglurant ADX-48621-dipraglurant	mGluR5 antagonists	Reduce dyskinesia	PD patient	Stocchi and others 2013
HD	MPEP	mGluR5 antagonist	Increases survival time Improves rotarod performance	R6/2 mouse	Schiefer and others 2004
HD	CDPPB	mGlu5 PAM	Prevents neuronal loss Decreases htt aggregation Ameliorates motor incoordination Rescues memory deficit	BACHD mouse	Doria and others 2015
HD	MTEP	mGlu5 NAM	Increases locomotor activity	HdhQ111/Q111 HD mouse	Ribeiro and others 2014
ID	CTEP	mGlu5 NAM	Prolongs lifespan Reduces long breath-holding Ameliorates inhibitory avoidance deficit	Fmr1 KO mouse	Tao and others 2016
RTT	CTEP	mGlu5 NAM	Improves lifespan	Mecp2 KO mice	Tao and others 2016
Ischemia	MPEP CHPG	mGluR5 antagonist mGluR5 agonist	Reduce infarct volume	MCAO rat	Bao and others 2001
Depression	MPEP MTEP GRN-529 Basimglurant DSR-98776	mGlu5 NAM	Antidepressant action	MDD rat MDD patient	Chaki and Fukumoto 2018