Acetyl Tetrapeptide-15 e tsoa ho Endomorphin-2 ka acetylation phetoho sebakeng sa eona sa N-terminal tyrosine masalla. Phetoho ena e khethehileng ea lik'hemik'hale e sebelisoa hangata ho ntlafatsa botsitso ba peptide kapa ho fetola tšebetso ea eona ea tlhaho.
Endomorphin-2 ka boeona ke agonist e ngotsoeng hantle ea nang le kamano e phahameng le khetho bakeng sa li-receptor tsa μ-opioid (MORWALOI) joalo ka litšobotsi tsa eona tse hlalosang. Ka lebaka la ho tšoana ha eona le motsoako ona oa motsoali, Acetyl Tetrapeptide-15 ho nahanoa hore e na le mesebetsi e batlang e tšoana ea tlhaho.
Ea mantlha, le ho fihlela joale e ikhethile, ts'ebeliso ea peptide ena ea acetylated e oela ka har'a indasteri ea litlolo – lihlahisoa tsa letlalo tse nang le kutloelo-bohloko e le mohlala o atileng haholo oa ts'ebeliso ea eona joalo ka motsoako o sebetsang.
Tatelano
Ac-Tyr-Pro-Phe-Phe-NH2
Nomoro ea CAS
928007-64-1
Foromo ea limolek'hule
C34H39N5O6
Boima ba Molek'hule
613.70 g/mol
Patlisiso ea Acetyl Tetrapeptide-15
Nts'etsopele ea acetyl tetrapeptide-15 e ikemiselitse ho phahamisa moeli oa thabo ea μ-opioid receptor-expressing neurons.; endorphin-joalo ka mekhoa e sebelisoang. Ho matlafatsa mamello ea letlalo ho mefuta e sa tšoaneng ea ka ntle le ho fokotsa ho ruruha, bohloko bo sa foleng esita le neuropathic e amanang le hyperreactivity ea letlalo ke phello e lakatsehang.
1.Ho fetola tokollo ea CGRP
CGRP (peptide e amanang le liphatsa tsa lefutso ea calcitonin) ke neuropeptide e matla ea pro-inflammatory. Li-neurons tsa kutlo lia e lokolla, vasodilation le bofubelu bo latelang / edema ke lipontšo tse peli tse tobileng tsa kutloisiso ena. Kutloelo-bohloko ea letlalo le likarabelo tse amanang le ho ruruha bonyane li kenella ka mokhoa o itseng ke CGRP.
Ts'ebetso ea moamoheli oa TRPV1 (capsaicin, mocheso, li-depolarizing agents kaofela li sebetsa e le lintho tse susumetsang) e lebisa tokollong ea eona. Motsoako oa setso Li-neurone tsa kutlo tse tšoaroang ka acetyl tetrapeptide-15 li bontšitse tšitiso e kholo ea capsaicin le Potassium chloride (KCl, kapa letsoai la potasiamo) e hlahisitse tokollo ea CGRP – phello e bapisoang le, kapa molemo hofeta, mohanyetsi ea tsebahalang oa TRPV1 capsazepine.
2.Ts'ebetso ea li-receptor tsa μ-Opioid
Ka tlhahlobo ea in vitro: Ka har'a mohlala oa ho susumetsa capsaicin, acetyl tetrapeptide-15 e tlameletsoe ka tlholisano ho li-receptor tsa μ-opioid ho li-neuron tse hlahisitsoeng. Mohanyetsi oa opioid naloxone o ile a sebelisoa ho tiisa tlamo ena.
Capsaicin ka boeona e tlama ho li-receptor tsa TRPV1, ho hlahisa khalsiamo e ngata; ho lokolloa ha CGRP ho latelang le matšoao a bohloko a latela ka lebaka leo. acetyl tetrapeptide-15 e fokolitse haholo tokollo ena ea CGRP e susumelitsoeng ke capsaicin, phello e thibelang ea naloxone e fanang ka tiiso e hlokahalang ea ho kenya letsoho ho amohelang.
Ho kenya tšebetsong li-receptor tsena ho lumella acetyl tetrapeptide 15 ho fetola hampe tšebetso ea methapo ea kutlo; pro-inflammatory neuropeptides (CGRP ke mohlala o motle) ka hona li lokolloa hanyane. Ho thibela ho ruruha ha methapo ea kutlo mohloling oa eona ke phello e khahlanong le ho ruruha, ho thoba ho ba e 'ngoe.
3.Thuto ea Tleliniki
Teko ea kliniki e sa boneng e le 'ngoe e ile ea lekola bokhoni ba acetyl tetrapeptide-15 ho fokotsa kutloelo-bohloko ea letlalo.. Keketseho e ntseng e eketseha ea tharollo ea capsaicin e ile ea sebelisoa lesapo la nasolabial (boemo bo sa thabiseng ke tekanyo ea thahasello), ka lerama la contralateral le sebetsang joalo ka taolo ea koloi.
Tšebeliso e phetoang ea peptide, ho 0.0015%, habeli ka letsatsi ka matsatsi a mane, e ile ea latela liphephetso tse ling tsa capsaicin, e bontšitse keketseho e hlakileng le e ka lekanngoang moeling oo.
Hajoale ts'ebeliso ea acetyl tetrapeptide-15 e ntse e lekanyelitsoe ho litlolo tsa litlolo.. Anti-sensitization ea mantlha ke seo e fanang ka sona; lihlahisoa tsa letlalo tse hlokolosi (ho fihlela joale bonyane) ela sena hloko.
Ho chesa le ho hlaba ho fokotsehile, le ho isa ntlheng, mefuta eohle ea ho se thabise kapa e haufi le ho tloaeleha ha kutlo ea letlalo e ka finyelloa. Li-analgesics tse ncha tsa sehlooho le li-anti-inflammatory agents ke mohato o latelang o utloahalang, le acetyl tetrapeptide-15 e na le monyetla ho saense ea dermatological kapa cosmetic nakong e tlang..
COA
HPLC
MOF
