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. 2012 Mar;10(1):12–48. doi: 10.2174/157015912799362805

Table 6.

Summary of Preclinical Studies Supporting a Role of mGluRs in Pain

Receptor Subtype Pharmacological Tool Effect References

Group I

mGluR1 A841720 (antagonist) ↓ CFA-induced pain in rats El-Kouhen et al. 2006;Zheng et al. 2005
↓ Mechanical allodynia in rats

A841720 ↓ Post-operative pain in rats Zhu et al. 2008
A794282
A794278
A850002 (antagonists)

CPCCOEt (antagonist) ↓ Formalin- induced pain in mice Bhave et al. 2001;Han and Neugebauer 2005
↓ Thermal hyperalgesia in mice
↓ Noxious stimulation- induced pain in rats

AIDA ↓ Formalin- induced pain in mice Lee et al. 2007;Varty et al. 2005;Zhang et al. 2002
LY456236 ↓ Thermal hyperalgesia in mice and rats
LY36738 (antagonists) ↓ Mechanical allodynia in rats

mGluR5 SIB1757 (antagonist) ↓ Thermal hyperalgesia in rats Dogrul et al. 2000

MPEP & MTEP (antagonists) ↓ Formalin- induced pain in mice Bhave et al. 2001;Vartyet al. 2005;Zhu et al. 2004;Lee et al. 2007;Walkeret al. 2001
↓ Post-operative pain in rats
↓Thermal hyperalgesia in mice
↓ Noxious stimulation- induced pain in rats
↓ Carrageenan- induced pain in mice
↓ CFA- induced pain in rats
↓ Touch-evoked allodynia in mice
↓ Mechanical allodynia in mice

Group II

LY354740 ↓ Carrageenan- induced pain in rats Simmons et al. 2002;Jones et al. 2005
LY379268 ↓ CFA-induced pain in rats
mGluR2/3 LY389795 (agonists) ↓ Formalin-induced pain in rats
↓ Mechanical allodynia in rats
↓ Thermal hyperalgesia in rats

APDC (agonist) ↓ Thermal-induced pain in rats Neugebauer and Carlton 2002;Yang and Gereau 2003
↓ Formalin-induced pain in rats
↓ Carrageenan- induced pain in mice
↓ CFA- induced pain in rats
↓ Thermal hyperalgesia in rats

Group III

mGluR4/7/8 l-AP4 (agonist) ↓ Mechanical allodynia in rats Chen and Pan 2005

ACPT-I (agonist) ↓ Carrageenan-induced pain in rats Goudet et al. 2008
↓ Vincristine-induced pain in rats

mGluR4 PHCCC (PAM) ↓ Carrageenan-induced pain in rats Goudet et al. 2008
↓ Vincristine-induced pain in rats

mGluR7 AMN082 (agonist) ↓ Carrageenan-induced pain in rats Palazzo et al. 2008

(S)-3,4-DCPG (agonist) ↓ Carrageenan-induced pain in rats Palazzo et al. 2008
↓ Vincristine-induced pain in rats

Abbreviations and symbols: ↓, decreased; CFA, complete Freund's adjuvant; NAM, negative allosteric modulator; PAM, positive allosteric modulator.

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