HTR2A

HTR2A
Identifikatori
Aliasi	HTR2A
Vanjski ID-jevi	OMIM: 182135 MGI: 109521 HomoloGene: 68073 GeneCards: HTR2A
Lokacija gena (čovjek) Hrom. Hromosom 13 (čovjek)[1] Bend 13q14.2 Početak 46,831,546 bp[1] Kraj 46,897,076 bp[1]
Obrazac RNK ekspresije Više referentnih podataka o ekspresiji
Ontologija gena Molekularna funkcija • 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding • G protein-coupled receptor activity • virus receptor activity • signal transducer activity • G-protein alpha-subunit binding • G protein-coupled serotonin receptor activity • serotonin binding • neurotransmitter receptor activity • GO:0001948, GO:0016582 vezivanje za proteine • GO:0032403 protein-containing complex binding Ćelijska komponenta • citoplazma • integral component of membrane • citosol • projekcija ćelije • membrana • cell body fiber • integral component of plasma membrane • dendritic shaft • Akson • soma • Kaveole • GO:0016023 citoplazmatska vezikula • ćelijska membrana • dendrit • glutamatergic synapse • integral component of postsynaptic membrane • integral component of presynaptic membrane Biološki proces • detection of mechanical stimulus involved in sensory perception of pain • release of sequestered calcium ion into cytosol • regulation of dopamine secretion • phospholipase C-activating serotonin receptor signaling pathway • urinary bladder smooth muscle contraction • positive regulation of MAP kinase activity • behavioral response to cocaine • positive regulation of cytosolic calcium ion concentration • positive regulation of kinase activity • positive regulation of phosphatidylinositol biosynthetic process • GO:0010260 starenje • cellular calcium ion homeostasis • Ćelijska smrt • Memorija • activation of phospholipase C activity • detection of temperature stimulus involved in sensory perception of pain • protein localization to cytoskeleton • Spavanje • positive regulation of vasoconstriction • positive regulation of cell population proliferation • negative regulation of potassium ion transport • positive regulation of ERK1 and ERK2 cascade • artery smooth muscle contraction • positive regulation of peptidyl-tyrosine phosphorylation • viral entry into host cell • phosphatidylinositol 3-kinase signaling • Nocicepcija • temperature homeostasis • GO:0022415 viral process • positive regulation of fat cell differentiation • positive regulation of glycolytic process • negative regulation of synaptic transmission, glutamatergic • GO:0072468 Transdukcija signala • chemical synaptic transmission • serotonin receptor signaling pathway • phospholipase C-activating G protein-coupled receptor signaling pathway • G protein-coupled receptor signaling pathway • GO:0035737 životinjsko ponašanje • regulation of synaptic vesicle exocytosis • G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger Izvori:Amigo / QuickGO
Ortolozi
Vrste	Čovjek	Miš
Entrez	3356	15558
Ensembl	ENSG00000102468	ENSMUSG00000034997
UniProt	P28223	P35363
RefSeq (mRNK)	NM_001165947 NM_000621 NM_001378924	NM_172812
RefSeq (bjelančevina)	NP_000612 NP_001159419 NP_001365853	NP_766400
Lokacija (UCSC)	Chr 13: 46.83 – 46.9 Mb	n/a
PubMed pretraga	[2]	[3]
Wikipodaci
Pogledaj/uredi – čovjek Pogledaj/uredi – miš

Receptor 5-HT_2A je podtip receptora5-HT₂ porodice serotononskih G protein-spregnutih receptora (GPCR).^[4] Recweptor 5-HT_2A je receptor ćelijske površine.^[5] 5-HT je skraćenica za 5-hidroksi-triptamin, koji je serotonin. Ovo je glavni podtip ekscitacijskog receptora među GPCR za serotonin, iako 5-HT_2A također može imati inhibitorni učinak^[6] na određenim područjima kao što su vizuelni i orbitofrontalni korteks.^[7] Ovaj receptor je prvi put zapažen po svom značaju kao meta serotonergični psihodelični lijekovi kao što su LSD i psilocibinska gljiva. Kasnije se vratio na vidjelo jer je utvrđeno da je barem djelomično posredovao u djelovanju mnogih antipsihotičnih lijekova, posebno atipskih.

Smanjena regulacija postsinapsnihih receptora 5-HT_2A je adaptivni proces izazvan hroničnom primjenom selektivnih inhibitora preuzimanja serotonina (SSRI) i atipskih antipsihotika. Samoubilački i na drugi način depresivni pacijenti imali su više receptora 5-HT_2A od normalnih pacijenata. Ovi nalazi ukazuju na to da je postsinapsna prekomjerna gustoća 5-HT_2A uključena u patogenezu depresije.^[8]

Paradoksalna podregulacija receptora 5-HT_2A može se primijetiti s nekoliko antagonista 5-HT _2A.^[9] Prema tome, umjesto tolerancije, od antagoniste 5-HT_2A očekivala bi se reverzna tolerancija. Međutim, na ovom mjestu postoji barem jedan antagonist za koji je pokazano da poboljšava receptore 5-HT_2A.^[10] Osim toga, nekoliko drugih antagonista možda neće uticati na broj receptora 5-HT_2A.^[11] Ipak, nadregulacija je prije izuzetak nego pravilo. Niti tolerancija niti odskok ne primjećuju se kod ljudi s obzirom na SWS koji promovira efekte antagonista 5-HT_2A.^[12]

1. ^ ^{a b c} GRCh38: Ensembl release 89: ENSG00000102468 - Ensembl, maj 2017
2. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
3. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
4. ^ Cook EH, Fletcher KE, Wainwright M, Marks N, Yan SY, Leventhal BL (august 1994). "Primary structure of the human platelet serotonin 5-HT_2A receptor: identify with frontal cortex serotonin 5-HT_2A receptor". Journal of Neurochemistry. 63 (2): 465–9. doi:10.1046/j.1471-4159.1994.63020465.x. PMID 8035173. S2CID 40207336.
5. ^ Kling A (2013). 5-HT2A: a serotonin receptor with a possible role in joint diseases (PDF). Umeå: Umeå Universitet. ISBN 978-91-7459-549-9.
6. ^ Martin P, Waters N, Schmidt CJ, Carlsson A, Carlsson ML (1998). "Rodent data and general hypothesis: antipsychotic action exerted through 5-HT_2A receptor antagonism is dependent on increased serotonergic tone". Journal of Neural Transmission. 105 (4–5): 365–96. doi:10.1007/s007020050064. PMID 9720968. S2CID 20944107.
7. ^ De Almeida RM, Rosa MM, Santos DM, Saft DM, Benini Q, Miczek KA (maj 2006). "5-HT(1B) receptors, ventral orbitofrontal cortex, and aggressive behavior in mice". Psychopharmacology. 185 (4): 441–50. doi:10.1007/s00213-006-0333-3. PMID 16550387. S2CID 33274637.
8. ^ Eison AS, Mullins UL (1996). "Regulation of central 5-HT_2A receptors: a review of in vivo studies". Behavioural Brain Research. 73 (1–2): 177–81. doi:10.1016/0166-4328(96)00092-7. PMID 8788498. S2CID 4048975.
9. ^ Yadav PN, Kroeze WK, Farrell MS, Roth BL (oktobar 2011). "Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo". The Journal of Pharmacology and Experimental Therapeutics. 339 (1): 99–105. doi:10.1124/jpet.111.183780. PMC 3186284. PMID 21737536.
10. ^ Rinaldi-Carmona M, Congy C, Simiand J, Oury-Donat F, Soubrie P, Breliere JC, Le Fur G (januar 1993). "Repeated administration of SR 46349B, a selective 5-hydroxytryptamine2 antagonist, up-regulates 5-hydroxytryptamine2 receptors in mouse brain". Molecular Pharmacology. 43 (1): 84–9. PMID 8423772.
11. ^ Gray JA, Roth BL (novembar 2001). "Paradoxical trafficking and regulation of 5-HT(2A) receptors by agonists and antagonists". Brain Research Bulletin. 56 (5): 441–51. doi:10.1016/s0361-9230(01)00623-2. PMID 11750789. S2CID 271925.
12. ^ Vanover KE, Davis RE (28. 7. 2010). "Role of 5-HT2A receptor antagonists in the treatment of insomnia". Nature and Science of Sleep. 2: 139–50. doi:10.2147/nss.s6849. PMC 3630942. PMID 23616706.