Na Cocer Peptides 
ukwezi gushize
INGINGO ZOSE N'AMAKURU Y’IBICURUZWA BITANZWE KURI URU RUBUGA BISANZWE KUBONA AMAKURU N'INTEGO Z'UBUREZI.
Ibicuruzwa byatanzwe kururu rubuga bigenewe gusa mubushakashatsi bwa vitro. Mu bushakashatsi bwa vitro (Ikilatini: * mu kirahure *, bisobanura mu bikoresho by'ibirahure) bikorwa hanze y'umubiri w'umuntu. Ibicuruzwa ntabwo ari imiti, ntabwo byemejwe n’ikigo cy’Amerika gishinzwe ibiryo n’ibiyobyabwenge (FDA), kandi ntigomba gukoreshwa mu gukumira, kuvura, cyangwa gukiza indwara iyo ari yo yose y’ubuvuzi, indwara, cyangwa indwara. Birabujijwe rwose n'amategeko kwinjiza ibyo bicuruzwa mumubiri wabantu cyangwa inyamaswa muburyo ubwo aribwo bwose.
Dermorphine ni peptide ikomeye ya opioide itandukanijwe nuruhu rwibinyabuzima bimwe na bimwe.
Uburyo bwa Dermorphine Ingaruka Zisesengura
Imikoranire na Opioid yakira
Dermorphine ikora cyane cyane ingaruka zayo zo gusesengura ikorana na μ-opioid reseptor (MOP). Reseptor ya μ-opioid ni umunyamuryango wingenzi wumuryango wa reseptor ya opioid kandi igira uruhare runini muguhindura ububabare. Dermorphine hamwe nibigereranirizo byayo birashobora guhuza cyane na reseptor ya MOP, bisa nurufunguzo rukwiranye nugufunga, bityo bigakora inzira yerekana ibimenyetso byinzira. ] Itera poroteyine G ihuza, igatera GTPγ [35S] guhuza, bityo igahindura ibimenyetso bifitanye isano, kandi amaherezo ikabuza kwanduza ububabare. Dermorphine kandi itera ERK1 / 2 fosifora, bikagira ingaruka ku mikorere y’ibinyabuzima ndetse no kugira uruhare mu kugenzura ingaruka zidakira.
Kubuza kwanduza ibimenyetso byububabare kurwego rwumugongo
Ubushakashatsi bwakozwe bwerekanye ko Dermorphine ibuza cyane kwanduza ibimenyetso by’ububabare ku rwego rwumugongo. Mu bushakashatsi bwakozwe, kwinjiza imitsi ya 0,16 mg / kg Dermorphine byatumye ubwiyongere bukomeye kandi burambye bwiyongera ku mbuto ya nociceptive flexion reflex ku bushake bw’abakorerabushake bazima, kandi iyi ngaruka yagaragaye no mu ngingo zifite ibikomere byuzuye by’umugongo, byerekana ko Dermorphine ibuza cyane kwanduza nociceptive ku rwego rwumugongo. Ubu buryo bwibikorwa bushobora kuba bufitanye isano nogutegeka kwa Dermorphin kurekura neurotransmitter kurekura uruti rwumugongo cyangwa ibikorwa byayo kuri neuron yumugongo. Uruti rw'umugongo rukora nk'ihuriro rikomeye ryo kwanduza ibimenyetso by'ububabare, kandi guhindura Dermorphin guhindura imikorere yabyo guhagarika neza kwanduza hejuru ibimenyetso by’ububabare mu bwonko, bityo bikagera ku ngaruka zo kubabaza.
Ibiranga ibikorwa byihariye bya reseptor
Nubwo naloxone ishobora kurwanya rwose ingaruka ziterwa na morphine na opioid, irashobora gusa igice (hafi 50%) guhindura ingaruka za Dermorphine zo kubuza kwifata nociceptive spinal reflexes. Ibi byerekana ko Dermorphine ikorana nitsinda ritandukanye ryakira uruti rwumugongo mugihe rutera analgesia, kandi uburyo bwibikorwa bitandukanye nubwa miti gakondo ya opioide. Ubu buryo bwibikorwa butanga inyungu zimwe murwego rwo gusesengura, nko kugabanya ingaruka zisanzwe zijyanye nibiyobyabwenge bya opioid.
Imikorere ya Analgesic ya Dermorphine mubushakashatsi bwinyamaswa
Analgesia Nziza muburyo bwinshi bw'inyamaswa
Muburyo butandukanye bwo kubabaza inyamaswa, Dermorphin yerekanye ingaruka zikomeye zo gusesengura. Mu bushakashatsi nka umurizo-flick, isahani ishyushye, umurizo wumurizo, formaline, hamwe na acide acide acide, ubuyobozi bwa intermeritoneal ya Dermorphin hamwe na peptide bifitanye isano nayo byagabanije inyamaswa kumva ububabare kandi byongera ububabare bwabo. Ubu bushakashatsi bwerekanye ububabare bwingeri zitandukanye nubwoko butandukanye, byemeza byimazeyo ubushobozi bwa analgesic bwa Dermorphin. Mu kizamini gishyushye, nyuma yo guha Dermorphine inyamaswa, igihe cyo gutinda kurigata amaguru cyangwa gusimbuka cyari kirekire cyane, byerekana ububabare bwatewe no gukurura ubushyuhe, bityo bikerekana ingaruka nziza za Dermorphine.
Kugereranya Inyungu Kuruta Ibindi Biyobyabwenge
Ugereranije n'imiti gakondo idakira nka morphine, Dermorphine igaragaza ibyiza byingenzi mubice bimwe. Mubyitegererezo byinyamanswa, nyuma yubuyobozi bwa interacerebroventricular, Dermorphin yerekanye ingaruka zihitamo kandi zikomeye kuruta morphine, hamwe nigihe kirekire cyibikorwa. Dermorphine tetrapepetides imwe ikomatanya nayo yerekanye ibikorwa byinshi byo gusesengura, hamwe nimbaraga zo gusesengura inshuro zigera ku 1.500 ninshuro 17 za morphine nyuma yubuyobozi bwimitsi cyangwa imitsi yo munsi yimbeba. Izi nyungu zitanga ibyiringiro byokoreshwa mubuvuzi bwa Dermorphine muri analgesia, birashoboka gukemura ibibazo byimiti gakondo idakira, nkibikorwa bidahagije byo kuvura cyangwa igihe bimara.
Ubushakashatsi no Gushyira mu bikorwa Ubushakashatsi bwa Dermorphine mu bantu
Ibisubizo byambere byubuvuzi
Mu 1985, igeragezwa ry’amavuriro ryateguwe, rigenzurwa na platbo ku ikoreshwa rya Dermorphine mu bubabare nyuma yo kubagwa ryerekanye ko Dermorphine yatanzwe hakoreshejwe inshinge za intrathecal yarushije cyane umwanya wa morbo na morfine (ikoreshwa nk'ikomatanyirizo) mu bijyanye no gukora neza. Ubu bushakashatsi bwibanze bwatanze ibimenyetso bifatika byerekana ko Dermorphine ikoreshwa mu kuvura indwara ya analgesia, ikagaragaza imbaraga zayo mu kuvura ububabare nyuma yo kubagwa.
Ibishoboka byo gusaba
Gucunga ububabare nyuma yo kubagwa: Ihahamuka ryo kubaga rishobora gutera ububabare bukabije nyuma yo kubagwa, bikagira ingaruka zikomeye ku gukira kw'abarwayi no ku mibereho yabo. Dermorphin yerekanye imbaraga mu kugabanya ububabare nyuma yo kubagwa mu bigeragezo byo kwa muganga hakiri kare byerekana ko ari uburyo bushya butanga imiti igabanya ubukana nyuma yo kubagwa. Ugereranije n'imiti gakondo yo kuvura nyuma yo kubagwa, uburyo bwihariye bwibikorwa nibyiza - nko kugabanya ibyago byo kwihanganira ibiyobyabwenge no guterwa - biha abarwayi igisubizo cyiza kandi cyiza cyo gusesengura.
Kuvura ububabare budashira: Ku barwayi bafite ububabare budakira, cyane cyane abafite ibisubizo bibi ku miti gakondo idakira cyangwa bafite ingaruka zikomeye, Dermorphine irashobora kuba uburyo bwiza bwo kuvura. Mu gucunga ububabare budakira ku barwayi ba kanseri, uburyo bwo kuvura buracyafite aho bugarukira. Kugaragara kwa Dermorphin bizana ibyiringiro bishya kuri aba baturage barwayi. Ingaruka zayo zimara igihe kirekire zirashobora kurwanya neza ububabare buhoraho kubarwayi ba kanseri kandi bikazamura imibereho yabo.
Ubuvuzi bwa Palliative: Muburyo bwo kuvura indwara, kugabanya ububabare bwabarwayi nicyo kintu cyambere. Dermorphin ifite imbaraga zo gusesengura ibintu bituma iba umukandida utanga ikizere cyo kugabanya ububabare bwanyuma bwubuzima mubuvuzi bwa palliative. Binyuze muburyo bukwiye bwo kuyobora no guhindura ibipimo, birashobora gufasha abarwayi kugabanya imibabaro no kongera ihumure mugihe cyanyuma cyubuzima.
Umwanzuro
Nibintu bifite uburyo bwihariye bwo gusesengura hamwe ningaruka zikomeye zo gusesengura, Dermorphin ifite ibyifuzo bitanga umusaruro muburyo bwo gucunga ububabare.
Inkomoko
[1] Giakomidi D, Inyoni MF, McDonald J, n'abandi. Isuzumabumenyi rya [Cys (ATTO 488) 8] Dermorphine-NH2 nk'igikoresho gishya cyo kwiga μ-opioid peptide yakira [J]. Ikibanza cya mbere, 2021.16 (4): e250011.DOI: 10.1371 / ikinyamakuru.pone.0250011.
[2] Hesselink J, Schatman M E. Kuvumbura imiti ishaje: ikibazo cyibagiwe na dermorphine kubabara nyuma yo kubagwa no kurwara [J]. Ikinyamakuru cyubushakashatsi bwububabare, 2018,11: 2991-2995.DOI: 10.2147 / JPR.S186082.
[3] Guzevatykh LS, Voronina TA, Emel'Ianova TG, n'abandi. Kugereranya kugereranya ibikorwa byo gusesengura dermorphine, [DPro6] -dermorphine, na tripeptide ya C-terminal [J]. Izv Akad Nauk Ser Biol, 2007 (5): 577-582. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=18038625&query_hl=1
[4] Sandrini G, Degli UE, Salvadori S, n'abandi. Dermorphine ibuza umugongo nociceptive flexion reflex mu bantu [J]. Ubushakashatsi bwubwonko, 1986,371 (2): 364-367. DOI: 10.1016 / 0006-8993 (86) 90376-8.
[5] Salvadori S, Marastoni M, Balboni G, n'abandi. Synthesis hamwe na opioid ibikorwa bya dermorphine tetrapeptides ifite D-methionine S-oxyde kumwanya wa 2 [J]. Ikinyamakuru cya chimie yubuvuzi, 1986,29 (6): 889-894.DOI: 10.1021 / jm00156a003.
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