Signal transduction histamine receptors

Leurs, R., Traiffort, E., Arrang, J. M. et al. (1994). Guinea pig histamine HI receptor. II. Stable expression in Chinese hamster ovary cells reveals the interaction with three major signal transduction pathways. J. Neurochem. 62, 519-27. 

FIGURE 14-6 Main signaling pathways for histamine receptors. Histamine can couple to a variety of G-protein-linked signal transduction pathways via its four different receptors. The Hj receptor activates the phosphatidylinositol turnover via Gq/11 proteins. The other receptors either positively (H2 receptor) or negatively (H3 and H4 receptor) regulate adenylyl cyclase activity via Gs and GUo protein activation respectively. Several additional signaling pathways have been described, which are not shown. Abbreviations PfP2, phosphatidylinositol 4,5-bisphosphate PIC, phospholipase C AC, adenylyl cyclase ATP, adenosine triphosphate cAMP, cyclic AMP PKC, protein kinase C PICA, protein kinase A. 

O Reilly M, Alpert R, Jenkinson S, Gladue RP, Foo S, Trim S, Peter B, Trevethick M, Fidock M Identification of a histamine H4 receptor on human eosinophils - role in eosinophil chemotaxis. J Recept Signal Transduct Res 2002 22 431-448. 

Presynaptic H3 receptors also are uniform in their signal transduction. They couple to Gi/o proteins and decrease the depolarization-induced release of neurotransmitters by inhibiting multiple calcium channels (e.g., Arrang et al. 1985 Schlicker et al. 1994 Endou et al. 1994 Brown and Haas 1999 see Stark et al. 2004). For comparison, the signal transduction of soma-dendritic H3 autoreceptors in histamin-ergic neurons also involves a pertussis toxin-sensitive G-protein with subsequent inhibition of N- and P-type Ca2+ channels (Takeshita et al. 1998). The few exceptions to this signal transduction pathway are discussed in the corresponding subsections below (see Sections 3.1, 3.3, and 3.9). 

H3 receptor activation attenuates the release of glutmate in several brain regions (Table 3), but an endogenous input to the receptors has not been demonstrated. In the dentate gyrus adenosine, acting at Ai receptors, also attenuated the release of glutamate and occluded further inhibition by histamine, presumably because a common signal transduction pathway (Brown and Haas 1999). 

Bakker RA, Timmerman H, Leurs R. Histamine receptors specific ligands, receptor biochemistry, and signal transduction. In Simons FER, ed. Histamine and Hi-antihistamines in allergic disease. 2nd Ed. New York Marcel Dekker, 2002 27-64. 

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