Reseptor histamin: Perbedaan antara revisi
Konten dihapus Konten ditambahkan
Tidak ada ringkasan suntingan |
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* [[Reseptor H3]] |
* [[Reseptor H3]] |
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* [[Reseptor H4]] |
* [[Reseptor H4]] |
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==Perbandingan== |
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==Comparison== |
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{| class="wikitable" |
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|+Reseptor histamin |
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! Reseptor !! Mekanisme !! Fungsi !! Antagonis |
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! [[histamine H1 receptor|H<sub>1</sub>]] |
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| [[Gq subunit|G<sub>q</sub>]] |
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*kontraksi [[ileum]] |
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*modulasi [[siklus sirkadian]] |
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*gatal |
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*vasodilatasi sistemik |
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*[[bronkokonstriksi]] (asma terinduksi alergi) |
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*[[H1 antagonist|H<sub>1</sub>-receptor antagonist]]s |
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**[[Difenhidramin]] |
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**[[Loratadin]] |
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**[[Setirizin]] |
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**[[Feksofenadin]] |
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**[[Klemastin]] |
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! [[histamine H2 receptor|H<sub>2</sub>]] |
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| [[gs subunit|G<sub>s</sub>]] <BR> ↑ [[cAMP|cAMP<sup>2+</sup>]] |
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*mempercepat ritme sinus |
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*stimulasi sekresi asam lambung |
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*relaksasi otot polos |
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*menghambat sintesis [[antibodi]], proliferasi sel T, dan produksi [[sitokin]] |
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*[[H2 antagonist|H<sub>2</sub>-receptor antagonist]]s |
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**[[Ranitidin]] |
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**[[Simetidin]] |
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**[[Famotidin]] |
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**[[Nizatidin]] |
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! [[histamine H3 receptor|H<sub>3</sub>]] |
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| [[gi subunit|G<sub>i</sub>]] |
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* menurunkan pelepasan [[asetilkolin]], [[serotonin]], dan [[norepinefrin]] di SSP |
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*autoreseptor presinaptik |
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*[[H3 antagonist|H<sub>3</sub>-receptor antagonists]] |
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**[[ABT-239]] |
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**[[Ciproxifan]] |
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**[[Clobenpropit]] |
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**[[Thioperamide]] |
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! [[histamine H4 receptor|H<sub>4</sub>]] |
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| [[gi subunit|G<sub>i</sub>]] |
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*memediasi kemotaksi sel mast.<ref name="pmid12626656">{{cite journal |vauthors=Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP | title = Histamine H<sub>4</sub> receptor mediates chemotaxis and calcium mobilization of mast cells | journal = J. Pharmacol. Exp. Ther. | volume = 305 | issue = 3 | pages = 1212–21 | year = 2003 | pmid = 12626656 | doi = 10.1124/jpet.102.046581 }}</ref> |
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*[[Histamine antagonist#H4-receptor antagonists|H<sub>4</sub>-receptor antagonists]] |
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**[[Thioperamide]] |
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**[[JNJ 7777120]] |
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There are several [[splice variant]]s of H<sub>3</sub> present in various [[species]]. Though all of the receptors are [[7-transmembrane]] [[g protein coupled receptor]]s, H<sub>1</sub> and H<sub>2</sub> are quite different from H<sub>3</sub> and H<sub>4</sub> in their activities. H<sub>1</sub> causes an increase in [[PIP2|PIP<sub>2</sub>]] [[hydrolysis]], H2 stimulates [[gastric acid]] secretion, and H3 mediates [[feedback inhibition]] of histamine. |
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==Referensi== |
==Referensi== |
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Revisi per 20 November 2016 10.30
Reseptor histamin adalah anggota reseptor terhubung-protein G dengan ligan alaminya yaitu histamin.[1]
Klasifikasi
Perbandingan
Comparison
| Reseptor | Mekanisme | Fungsi | Antagonis |
|---|---|---|---|
| H1 | Gq |
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| H2 | Gs ↑ cAMP2+ |
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| H3 | Gi |
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| H4 | Gi |
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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.
Referensi
- ^ 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.