TABLE 4

Site of action for pharmacological agents acting on group II and group III mGlu receptors in the periphery

This table does not include studies performed in sensory cells.

AgentSite of ActionEffectReferences
Group II Agonists
    4C3HPGThymic cell lineReduction of forskolin-induced increase of cAMPStorto et al., 2000a
    APCDThymic cell lineReduction of forskolin-induced increase of cAMPStorto et al., 2000a
    DCG-IVCartilageInhibited mineralizationWang et al., 2005
    L-CCG-1Pancreatic β cellsIncreased release of insulinBrice et al., 2002
Group II antagonists
    LY341495Tumor cellsInhibition of cell proliferation and number of tumor aggregatesArcella et al., 2005; D'Onofrio et al., 2003; Iacovelli et al., 2006
    PCCG-4Thymic cell lineInhibition of 4C3HPG-induced effectStorto et al., 2000a
Group III Agonists
    ACPT-IOsteoclastsReduction in KCl-evoked secretion of glutamate and bone degradation productsMorimoto et al., 2006
Pancreatic cellsInhibition of glucagon secretion at low concentrations of glucoseUehara et al., 2004
    AMN082aColonIncreased fecal water content in vivo and electrolyte secretion in vitroJulio-Pieper et al., 2010
    DCPGColonIncreased motilityTong and Kirchgessner, 2003
Pancreatic cellsInhibition of glucagon secretion at low concentrations of glucoseUehara et al., 2004
    l-AP4DuodenumIncreased intracellular pH and mucus gel thicknessAkiba et al., 2009
Tumor cellsIncreased cell invasivenessChang et al., 2005
Pancreatic β cellsIncreased release of insulin at low concentrations of glucoseBrice et al., 2002
LymphocytesProduction of ROSBoldyrev et al., 2004
Endothelial cellsIncreased paracellular permeabilityCollard et al., 2002
OsteoblastsInhibited accumulation of cAMP induced by forskolin and parathyroid hormoneHinoi et al., 2001
CartilageInhibited mineralizationWang et al., 2005
Embryonic bodiesIncreased expression of markers for cell differentiationCappuccio et al., 2006
    PPGColonIncreased motilityTong and Kirchgessner, 2003
Pancreatic cellsInhibition of glucagon secretion at low concentrations of glucoseUehara et al., 2004
Group III Antagonists
    CPPGColonInhibits motility and PPG-induced increase in motilityTong and Kirchgessner, 2003
Endothelial cellsAttenuated glutamate-mediated increases in paracellular permeabilityCollard et al., 2002
OsteoblastsPrevention of l-AP4 effectHinoi et al., 2001
OsteoclastsBlockade of effects induced by ACPT-IMorimoto et al., 2006
Pancreatic cellsPrevention of Glu-induced inhibition of glucagon secretionUehara et al., 2004
    MAP4DuodenumPrevention of glutamate-induced alkalinization and mucus secretionAkiba et al., 2009
Bone stromal cellsInhibition of Glu-induced reduction of NOS activity and intracellular Ca2+ levelsForeman et al., 2005
    MSOPEmbryonic bodiesInhibition of l-AP4-induced expression of markers for cell differentiationCappuccio et al., 2006
  • ACPT-I, (1S,3R,4S)-1-aminocyclopentane-1,3,4-tricarboxylic acid; L-CCG-1, (2S,1′S,2′S)-2-(carboxycyclopropyl)glycine; MSOP, (R,S)-α-methylserine-O-phosphate; NOS, nitric-oxide synthase; PCCG-4, (2S,1′S,2′S,2′R)-2-(2′-carboxy-3′phenylcyclopropyl)glycine; PPG, (R,S)-phosphonophenylglycine.

  • a Specific for mGlu7 receptor.