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Histamine Receptor

Histamine is synthesized in the tuberomamillary nucleus (TMN) neurons from histidine by the specific enzyme histidine decarboxylase (HDC). Four histamine receptors, which are GPCRs, have been cloned (H1eH4R). H1R, H2R and H3R are expressed in distinctive patterns in the brain and all three receptor types are highly expressed in the hypothalamus. The H1Rs mediate excitatory actions on central neurons usually by recruiting Gq/11 and PLC, which leads to the formation of the two second messengers, diacylglycerol (DAG) and inositol-1,4,5-triphosphate (Ins(1,4,5)P3) and Ca2þ release from internal stores. The H2Rs couple to Gs, adenylyl cyclase (AC) and PKA, which phosphorylates proteins and activates the transcription factor cyclic-AMP-response element (CRE)-binding protein (CREB). The H3Rs couple to Gs, adenylyl cyclase (AC) and PKA, which phosphorylates proteins and activates the transcription factor cyclic-AMP-response element (CRE)-binding protein (CREB).

References

1.Tabarean IV. Neuropharmacology. 2016;106:13–19.

GPCR/G Protein

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