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. Author manuscript; available in PMC: 2010 Jul 21.
Published in final edited form as: Nat Rev Drug Discov. 2009 Jan;8(1):41–54. doi: 10.1038/nrd2760

Table 2.

Potential indications for allosteric modulators of mGluRs

compound structure compound
name
(reference)		 mglur
subtype		 study data
Pain
graphic file with name nihms211388t1.jpg CPCCOEt
(27)		 1 NAM 1st allosteric modulator
of an mGluR
Anxiety, fragile X syndrome, GERD, chronic pain, depression, migraine
graphic file with name nihms211388t2.jpg SIB-1757
(28)		 5 NAM One of the first
allosteric modulators
of mGluR 5
graphic file with name nihms211388t3.jpg SIB-1893
(28)		 5 NAM One of the first
allosteric modulators
of mGluR 5
graphic file with name nihms211388t4.jpg MPEP
(29)		 5 NAM Anxiolytic activity in
animal models

Established mGluR
theory of fragile X
syndrome
graphic file with name nihms211388t5.jpg MTEP (30) 5 NAM Anxiolytic activity in
animal models
graphic file with name nihms211388t6.jpg Fenobam
(34)		 5 NAM Anxiolytic activity in
animal models

Efficacious in clinical
trials in humans for
anxiety and GERD
graphic file with name nihms211388t7.jpg M-5MPEP
(41)		 5 Partial
antagonist		 One of the first partial
mGluR5 antagonists
graphic file with name nihms211388t8.jpg Br-5MPEPy
(41)		 5 Partial
antagonist		 One of the first partial
mGluR5 antagonists
Schizophrenia, cognition, extinction
graphic file with name nihms211388t9.jpg DFB (48) 5 PAM Acts at MPEP site
graphic file with name nihms211388t10.jpg CDPPB (51) 5 PAM Acts at MPEP site

Antipsychotic-like activity in
animal models
graphic file with name nihms211388t11.jpg ADX47273 (56) 5 PAM Acts at MPEP site

Antipsychotic-like and
cognition-enhancing activity
in animal models
Anxiety disorders, schizophrenia
graphic file with name nihms211388t12.jpg LY354740 (58) 2/3
agonist		 Anxiolytic and antipsychotic
activity in animal models
graphic file with name nihms211388t13.jpg LY341495 2/3
antagonist		 Anxiolytic and an tipsychotic
activity in animal models
graphic file with name nihms211388t14.jpg LY487379 (66) 2 PAM Anxiolytic and antipsychotic
activity in animal models
graphic file with name nihms211388t15.jpg BINA (70) 2 PAM Anxiolytic and an tipsychotic
activity in animal models
Parkinson’s disease, movement disorders
graphic file with name nihms211388t16.jpg (−)-PHCCC (86, 88) 4 PAM Robust activity in rodent
models of PD
graphic file with name nihms211388t17.jpg VU0155041 (87) 4 PAM/
Allosteric
agonist		 Robust activity in rodent
models of PD

GERD, gastroesophageal reflux disease; mGluR, metabotropic glutamate receptor; NAM, negative allosteric modulator; PAM, positive allosteric modulator; PD, Parkinson’s disease.