Clinical uses of histaminergic ligands according to their molecular mechanisms of action: current, proposed, and nontraditional
H1R | H2R | ||||||
---|---|---|---|---|---|---|---|
Molecular Mechanism of Action | Therapeutic Use | Pharmacological Effect | Reference | Molecular Mechanism of Action | Therapeutic Use | Pharmacological Effect | Reference |
Current | Antiallergic | Bakker et al. (2001), Panula et al. (2015) | Gs/AC/cAMP inhibition | Current | Gastric acid secretion regulation | Panula et al. (2015) | |
Gq/11 activity blockade; NF-κB inhibition | Repositioning | Analgesia; neurodegenerative disorders; sleep disorders; stress induced hypertension | Krystal et al. (2011), de Almeida et al. (2015), Shan et al. (2015), Apolloni et al. (2016), Rocha et al. (2016), Stein et al. (2016) | Repositioning | Chronic heart failure; diabetes; colorectal cancer | Pantziarka et al. (2014), Leary et al. (2016), Pini et al. (2016) | |
Biased agonism; GR crosstalk | Nontraditional | Neuroprotection; anti-inflammatory potentiation | Moniri et al. (2004), Zappia et al. (2015) | Biased agonism | Nontraditional | Gastric acid secretion rebound; AML treatment | Reher et al. (2012a,b), Alonso et al. (2014, 2015) |
NF-κB, nuclear factor-κB.