Reseptor histamin

Reseptor histamin adalah anggota reseptor terhubung-protein G dengan ligan alaminya yaitu histamin.^[1]

Klasifikasi

Reseptor histamin
Reseptor	Mekanisme	Fungsi	Antagonis
H₁	G_q	kontraksi ileum modulasi siklus sirkadian gatal vasodilatasi sistemik bronkokonstriksi (asma terinduksi alergi)	H₁-receptor antagonists Difenhidramin Loratadin Setirizin Feksofenadin Klemastin
H₂	G_s ↑ cAMP²⁺	mempercepat ritme sinus stimulasi sekresi asam lambung relaksasi otot polos menghambat sintesis antibodi, proliferasi sel T, dan produksi sitokin	H₂-receptor antagonists Ranitidin Simetidin Famotidin Nizatidin
H₃	G_i	menurunkan pelepasan asetilkolin, serotonin, dan norepinefrin di SSP autoreseptor presinaptik	H₃-receptor antagonists ABT-239 Ciproxifan Clobenpropit Thioperamide
H₄	G_i	memediasi kemotaksi sel mast.^[2]	H₄-receptor antagonists Thioperamide JNJ 7777120

There are several splice variants of H₃ present in various species. Though all of the receptors are 7-transmembrane g protein coupled receptors, H₁ and H₂ are quite different from H₃ and H₄ in their activities. H₁ causes an increase in PIP₂ hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine.

^ Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.
^ Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP (2003). "Histamine H₄ receptor mediates chemotaxis and calcium mobilization of mast cells". J. Pharmacol. Exp. Ther. 305 (3): 1212–21. doi:10.1124/jpet.102.046581. PMID 12626656.