TABLE 1

Histamine H1R and H2R: signaling pathways, receptor crosstalk, and ligands

SignalingH1RH2R
Pathway, Ligand, or ReceptorReferencePathway, Ligand, or ReceptorReference
Main signaling pathway involvedGq/11/PLC/Ca2+/PKC; Rac, RhoAGutowski et al. (1991), Notcovich et al. (2010)Gs/AC/PKAPanula et al. (2015)
Other signaling pathways regulatedGi/0; PLA2; AC/cAMP; NF-κBSnider et al. (1984), Leurs et al. (1994), Seifert et al. (1994), Bakker et al. (2001), Prast and Philippu (2001) Gq/11; PLA2; ERK1/2; PI3KLeopoldt et al. (1997), Mettler et al. (2007), Bonini et al. (2011), Luo et al. (2013), Alonso et al. (2016)
Classic reference ligandMepyramineSadek and Stark (2016)IodoaminopotentidineHirschfeld et al. (1992)
Biased ligands(−) trans-PAT; (±) cis-PABMoniri et al. (2004)Famotidine; cimetidine; tiotidine; ranitidineAlonso et al. (2014, 2015)
Crosstalk with other receptorsATP receptor; GRFitzsimons et al. (2004), Zappia et al. (2015)β-adrenergic receptor; calcitonin receptor; PGE2 receptorMonczor et al. (2003), Tubio et al. (2010)
  • NF-κB, nuclear factor-κB; PGE2, prostaglandin E2; PI3K, phosphoinositide 3-kinase; PKA, protein kinase A; PKC, protein kinase C; PLA, phospholipase A.