PE-22-28 ke analoge ea maiketsetso ea spadin, e bonts'ang botsitso le bokhabane bo ntlafalitsoeng ha e bapisoa le ea pele.
Ho tloha lipatlisisong tsa TREK-1 (KCNK2) mocha – setho sa kanale ea potassium ea pore tse peli (K2P) lelapa – e laola mekhoa e mengata ea fisioloji; neural excitability ke e 'ngoe ea tse thehiloeng hantle, mmoho le temoho ya bohloko, khatello ea maikutlo, le mefuta e sa tšoaneng ea neuroprotection.
Lithuto tsa pele li thehiloe sortilin joalo ka protheine e feto-fetohang e amang ts'ebetso ea TREK-1.
Liphuputso tse ling tse latelang li ile tsa hlakisa hore phello ena e etsahala ka sortilin e lokollang propeptide (PE) ho kena mading, qetellong e thibela phetiso ka mocha.
PE-22-28 ka boeona ke peptide ea maiketsetso e nkiloeng ho petsoha le ho fetola karolo ea mantlha e sebetsang ea propeptide ena..
Botsitso bo phahameng bo bonoa ho feta spadin, ka ts'ebetso e bolokiloeng nako e telele 23 lihora.
Liteko tsa bongaka li ntse li tsoela pele, empa lipontšo tsohle li supa molokong o mocha oa lithethefatsi tse reretsoeng ho tepella maikutlo, bohloko bo sa foleng le mathata a amanang le methapo ea kutlo.
Tatelano
Gly-Val-Ser-Trp-Gly-Leu-Arg
Nomoro ea CAS
1801959-12-5
Foromo ea limolek'hule
Setšoantšo sa C35H55N11O9
Boima ba Molek'hule
773.8930
Lipatlisiso tse amanang le PE22-28
1.Therapeutic Profile le Selection
Phello ea phekolo ea ho tepella maikutlong e feta ka ho khetheha tsohle tse kileng tsa ithutoa TREK-1 e thibelang li-antidepressants.; khatello e tšoailoeng ea bonyane letšoao le le leng la matšoao a tepeletseng a hlahang nakong ea matsatsi a mane, litla-morao ho ba sieo ka ho feletseng.
Litlamorao tsa neuroprotective li boetse li bonoa, libaka tse nyane tsa cerebral infarction le ntlafatso (ho isa bohōleng bo itseng bo ka khutlisoa) tikoloho ea methapo ea kutlo ho ba liphetho tse ka lekanngoang tse peli.
Khetho e phahameng e etsa hore PE-22-28 e be template e haufi e phethahetseng bakeng sa kalafo ea nakong e tlang ea TREK-1..
2.Liphello tsa ho tepella maikutlo
Thibelo ea likanale tsa TREK-1 (joalokaha ho boletsoe ka holimo) ke mochine o ka sehloohong.
Depolarization ea lera la neuronal ka ho eketseha ha thabo le ntlafatso ea phello ea polasetiki ea synaptic, ke eona e khutlisang likarolo tse ngata tsa pathological tsa khatello ea maikutlo.
Ho khutsufatsa ka potlako nako ea ho se sisinyehe mefuteng e mengata ea liphoofolo ke pontšo ea katleho e bontšitsoeng.
TREK-1 litoeba tse kokotang ka ho eketsehileng netefatsa sehokelo se tobileng le ho itšetleha ka mocha.
3.Liphello tsa Analgesic
Bohloko bo sa foleng hangata bo amahanngoa le ho tsosoa ho sa tloaelehang ha methapo ea kutlo.
Liteishene tsa TREK-1 li hlahisoa haholo ho li-neurone tsa mantlha tsa kutlo ka har'a litsela tse tsamaisang bohloko; mokokotlo oa motso oa ganglia (DRG) le lenaka la mokokotlo ea lesapo la mokokotlo e le mehlala e meholo.
Ts'ebetso ea bona e sebetsa e le mofuta oa taolo e mpe ea matšoao a bohloko.
Ho se sebetse kapa ho thibeloa ho hoholo ha likanale tsena ho lebisa ho pherekano e feteletseng e ikhethileng litseleng tse fapaneng tsa bohloko. – ho kenngoa le tlhokomelo e latelang ea bohloko bo sa foleng e le liphello tse tobileng tsa sena.
PE-22-28 ka katleho e tsamaisa mosebetsi oa likanale tsa calcium tse nang le voltage (Lisebelisoa tsa VGCC) le ka tekanyo e kgolo Li-receptor tsa NMDA, ka ho thefula methapo ena ea kutlo.
Ho hlophisa bocha thabo ea potoloho eohle e amanang le neural, a ‘ho tsosolosa’ ho tloha boemong ba pathologically hyper-excited ke phello ea ho qetela.
Liteko tsa kliniki li bonts'itse bophahamo bo boholo ba menyako ea bohloko ba mochini le mocheso (bakeng sa bonyane mefuta ea likotsi tse hatellang tsa bohloko, sciatica e le mohlala oa thuto ea mohlala) hammoho le allodynia e fokotsehileng le 'nete hyperalgesia.
4.Liphello tsa Neuroprotective
Litlamorao tse tlalehiloeng morao tjena tsa neuroprotective tsa PE-22-28 ha li so amoheloe hohle, empa mekhoa ea ho koala mecha ea ion e bontša mofuta o mong oa tšireletso nakong ea karolo e matla ea kotsi ea tsamaiso ea methapo.
Nako e telele, ho phahamisa neurotrophic factor poleloana, litsela tse fapaneng tsa ho pholoha le ho thibela apoptosis kaofela ho lumeloa e le karolo ea ketso ea eona.
Mekhoa e nepahetseng ea li-neuroprotective e ntse e tla hlalosoa ka botlalo, empa bopaki bo fana ka maikutlo a hore PE-22-28 bonyane e na le "neuroprotective" e itseng.
COA
HPLC
MOF
