TABLE 2

Clinical uses of histaminergic ligands according to their molecular mechanisms of action: current, proposed, and nontraditional

H1RH2R
Molecular Mechanism of ActionTherapeutic UsePharmacological EffectReferenceMolecular Mechanism of ActionTherapeutic UsePharmacological EffectReference
CurrentAntiallergicBakker et al. (2001), Panula et al. (2015) Gs/AC/cAMP inhibitionCurrentGastric acid secretion regulationPanula et al. (2015)
Gq/11 activity blockade; NF-κB inhibitionRepositioningAnalgesia; neurodegenerative disorders; sleep disorders; stress induced hypertensionKrystal et al. (2011), de Almeida et al. (2015), Shan et al. (2015), Apolloni et al. (2016), Rocha et al. (2016), Stein et al. (2016)RepositioningChronic heart failure; diabetes; colorectal cancerPantziarka et al. (2014), Leary et al. (2016), Pini et al. (2016)
Biased agonism; GR crosstalkNontraditionalNeuroprotection; anti-inflammatory potentiationMoniri et al. (2004), Zappia et al. (2015)Biased agonismNontraditionalGastric acid secretion rebound; AML treatmentReher et al. (2012a,b), Alonso et al. (2014, 2015)
  • NF-κB, nuclear factor-κB.