Oksitocinski receptor, ili , je protein koji dejstvuje kao receptor za hormon i neurotransmiter oksitocin.[1][2] Kod ljudi, oksitocinski receptor je kodiran genom.[3][4], koji je lokalizovan na ljudskom hromozomu .[5]
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Затвори
protein pripada familiji G-protein spregnutih receptora, specifično ,[1] i dejstvuje kao receptor za oksitocin. Njegova aktivnost je posredovana G proteinima koji aktiviraju više različitih sistema sekundarnih glasnika.[6][7]
Oksitocinski receptori su izraženi u mioepitelijalnim ćelijama mlečnih žlezdi, i u miometrijumu i endometrijumu uterusa na kraju trudnoće. Sistem oksitocina ima važnu ulogu indukovanja uterinskih kontrakcija tokom porođaja i izbacivanja mleka.
Oksitocinski receptori su takođe prisutni u centralnom nervnom sistemu. Ti receptori modulišu više odlika ponašanja, poput stresa i anksioznosti, socijalne memorije i prepoznavanja, seksualnog i agresivnog ponašanja, druženja (afilijacije) i materinskog ponašanja.[8][9][10]
Ko nekih sisara, oksitocinski receptori su takođe nađeni u bubrezima i srcu.
Nekoliko selektivnih liganda oksitocinskih receptora je nedavno bilo razvijeno, ali značajna sličnost između oksitocinskog i srodnog vazopresinskog receptora onemogućava visoku selektivnost.[11][12]
Agonisti
- Peptidi
- Non-peptidni
Antagonisti
- Peptid
- Non-peptidni
- [16][17]
- -L-371,257 (CAS# 162042-44-6)}-[18][19] – periferno selektivan (npr. slaba penetracija moždano-krvne barijere, malo centralnih efekata)[20]
- – centralno antagonist aktivan nakon periferne administracije
Simmons CF Jr; Clancy, TE; Quan R; Knoll, JH (1995). „The oxytocin receptor gene (OXTR) localizes to human chromosome 3p25 by fluorescence in situ hybridization and PCR analysis of somatic cell hybrids”. Genomics. 26 (3): 623—5. ISSN 0888-7543. PMID 7607693. doi:10.1016/0888-7543(95)80188-R. Gimpl, G.; Reitz, J.; Brauer, S.; Trossen, C. (2008). „Oxytocin receptors: Ligand binding, signalling and cholesterol dependence”. Advances in Vasopressin and Oxytocin — from Genes to Behaviour to Disease. Progress in Brain Research. 170. стр. 193—204. ISBN 9780444532015. PMID 18655883. doi:10.1016/S0079-6123(08)00417-2. Veenema AH, Neumann ID (2008). „Central vasopressin and oxytocin release: regulation of complex social behaviours”. Advances in Vasopressin and Oxytocin — from Genes to Behaviour to Disease. Progress in Brain Research. 170. стр. 261—76. ISBN 9780444532015. PMID 18655888. doi:10.1016/S0079-6123(08)00422-6. Chini B, Manning M (2007). „Agonist selectivity in the oxytocin/vasopressin receptor family: new insights and challenges”. Biochemical Society Transactions. 35 (Pt 4): 737—41. PMID 17635137. doi:10.1042/BST0350737. Manning M, Stoev S, Chini B, Durroux T, Mouillac B, Guillon G (2008). Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Progress in Brain Research. 170. стр. 473—512. PMID 18655903. doi:10.1016/S0079-6123(08)00437-8. Pitt GR, Batt AR, Haigh RM, Penson AM, Robson PA, Rooker DP, Tartar AL, Trim JE, Yea CM, Roe MB (2004). „Non-peptide oxytocin agonists”. Bioorganic & Medicinal Chemistry Letters. 14 (17): 4585—9. PMID 15357997. doi:10.1016/j.bmcl.2004.04.107. Rahman Z, Resnick L, Rosenzweig-Lipson SJ, Ring RH,"Methods of treatment using oxytocin receptor agonists", US patent application 2007/0117794, published 24. 5. 2007. , assigned to Wyeth Corp Ring RH, Schechter LE, Leonard SK, Dwyer JM, Platt BJ, Graf R, Grauer S, Pulicicchio C, Resnick L, Rahman Z, Sukoff Rizzo SJ, Luo B, Beyer CE, Logue SF, Marquis KL, Hughes ZA, Rosenzweig-Lipson S (2009). „Receptor and behavioral pharmacology of WAY-267464, a non-peptide oxytocin receptor agonist”. Neuropharmacology. 58 (1): 69—77. PMID 19615387. S2CID 8592340. doi:10.1016/j.neuropharm.2009.07.016. Williams PD, Anderson PS, Ball RG, Bock MG, Carroll L, Chiu SH, Clineschmidt BV, Culberson JC, Erb JM, Evans BE (1994). „1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor”. Journal of Medicinal Chemistry. 37 (5): 565—71. PMID 8126695. doi:10.1021/jm00031a004. Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF (1995). „1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist”. Journal of Medicinal Chemistry. 38 (23): 4634—6. PMID 7473590. doi:10.1021/jm00023a002. Wyatt PG, Allen MJ, Chilcott J, Foster A, Livermore DG, Mordaunt JE, Scicinski J, Woollard PM (2002). „Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives”. Bioorganic & Medicinal Chemistry Letters. 12 (10): 1399—404. PMID 11992786. doi:10.1016/S0960-894X(02)00159-2. Ring RH, Malberg JE, Potestio L, Ping J, Boikess S, Luo B, Schechter LE, Rizzo S, Rahman Z, Rosenzweig-Lipson S (2006). „Anxiolytic-like activity of oxytocin in male mice: behavioral and autonomic evidence, therapeutic implications”. Psychopharmacology (Berlin). 185 (2): 218—25. PMID 16418825. S2CID 13647805. doi:10.1007/s00213-005-0293-z.
- „Symbol Report: OXTR”. Human Geneome Organization Gene Nomenclature Committee. Архивирано из оригинала 18. 06. 2010. г. Приступљено 11. 10. 2010.
- „Vasopressin and Oxytocin Receptors: OT”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 03. 03. 2016. г.
- Caldwell HK, Young WS 3rd (2006). „Oxytocin and Vasopressin: Genetics and Behavioral Implications”. Ур.: Lajtha, Abel; Ramon Lim. Handbook of Neurochemistry and Molecular Neurobiology (3rd изд.). Berlin: Springer. стр. 573—607.