Disorders in which targeting mGlu receptors may be beneficial

Disorder/pathological conditionDesired EffectPotential TargetsReferences
ConstipationIncrease in fecal water contentmGlu7 activationJulio-Pieper et al., 2010
Increase in colonic motilitymGlu8 activationTong and Kirchgessner, 2003
DiabetesReduction of glucagon productionmGlu4 activationUehara et al., 2004
Duodenal ulcerIncrease in pH, mucus gel thicknessmGlu1, mGlu5 and mGlu4 activationAkiba et al., 2009
MedulloblastomaReduction in cell proliferationmGlu4 activationIacovelli et al., 2006
OsteoporosisDecrease in bone resorptionmGlu8 activationMorimoto et al., 2006
Brain gliomaReduction in cell proliferationmGlu2/3 inhibitionD'Onofrio et al., 2003
Colorectal carcinomaDecrease in cell survival and invasivenessmGlu4 inhibitionChang et al., 2005
Improved response to other chemotherapiesmGlu4 inhibitionYoo et al., 2004
Diabetes (type II)Reduction of insulinemiamGlu5 inhibitionStorto et al., 2006
Drug induced liver damageDecrease in necrosis and production of ROSmGlu5 inhibitionStorto et al., 2003
Gastroesophageal refluxaDecrease in frequency and intensity of reflux episodesmGlu5 inhibitionFrisby et al., 2005; Keywood et al., 2009
Hypoxia induced liver damageDecrease in cell damage and deathmGlu5 inhibitionStorto et al., 2004
MelanomaReduction in cell proliferationmGlu1 inhibitionShin et al., 2008
Oral squamous cell carcinomaDecrease in cell migration and invasivenessmGlu5 inhibitionPark et al., 2007
PruritusPrevention or treatment of itchingmGlu1 inhibitionGasparini and Spooren, 2007
SepsisDecrease in proinflammatory cytokinesmGlu1 inhibitionPacheco et al., 2006
  • a In phase I clinical trial.