Table 1 mGlu receptor therapeutic areas and prototypic allosteric modulators.

From: Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants

Group Subtype Therapeutic Area Prototypic NAMs Prototypic PAMs
I mGlu1 NAMs: Fragile X syndrome, anxiety, Alzheimer’s disease, schizophrenia, pain and addiction1,15,16 FITM, CPCCOEt Ro67-7476
mGlu5 NAMs: Fragile X syndrome, anxiety, chronic pain, depression, migraine, Parkinson’s disease, gastroesophageal reflux disease, epilepsy and addiction1,4,5,13,14,15,16 MPEP, Mavoglurant, Fenobam CPPHA, CDPPB
PAMs: Anxiety, Huntington’s disease, schizophrenia1,4,5,15,16   
II mGlu2 PAMs: Addiction, Alzheimer’s disease, anxiety, depression, pain, schizophrenia1,4,5,15,16 RO5488608 BINA, LY487379
mGlu3 NAMs: Depression1,16 ML337
PAMs: Alzheimer’s disease, pain, anxiety1   
III mGlu4 PAMs: Schizophrenia, pain, multiple sclerosis, Parkinson’s disease4,5,11,12,15,16 PHCCC
mGlu6 Congenital stationary night blindness1,5
mGlu7 NAMs: depression, anxiety1,15,16,20 MMPIP AMN082