NA Semax Amidate shine ingantaccen tsarin analog na ban ji ba. Yana da N-terminally acetylated da C-terminally amidated wanda aka samu na Semax peptide, wanda ke adana ainihin jerin.
Wannan gyare-gyare na wucin gadi yana inganta juriya na sarkar peptide da exo- da kuma endopeptidases (misali leucine aminopeptidase), tsawaita rabin rayuwarsa da kusan 30 mintuna idan aka kwatanta da ainihin Semax, tare da wani overall duration na mataki na 6-12 hours.
Hakanan yana haɓaka kwanciyar hankali a cikin ɗaki da ƙimar ƙwayar mucosal na hanci, don haka tabbatar da mafi aminci shigar azzakari cikin farji shingen kwakwalwar jini (BBB) da kuma ci gaba da kiyaye inganci maida hankali gradient a cikin nama na kwakwalwa.
Babban tsarin sa ya ta'allaka ne a cikin daidaitawar hanyoyi da yawa na tsarin juyayi na tsakiya aiki.
Na farko kuma mafi mahimmanci, NA Semax Amidate yana aiki azaman mai ƙarfi mai ƙarfi na neurotrophic factor da aka samu a kwakwalwa (BDNF), wanda hakan ke kara inganta rayuwar neuronal, girma axonal, synaptic filastik kuma dogon lokaci potentiation (LTP) - tushen kwayoyin halitta don koyo da ƙwaƙwalwa.
Haka kuma,NA Semax Amidate yana ƙarfafa dopaminergic, serotonergic, da noradrenergic neurotransmission, ta haka ingantawa prefrontal bawo ayyuka na zartarwa, gami da zabar hankali da memory aiki iya aiki.
NA Semax Amidate kuma yana nuna mahimman tasirin neuroprotective ta hanyar hana sakin cytokine mai kumburi., rage oxidative danniya lalacewa, da kuma tabbatar da yuwuwar mitochondrial membrane.
Yana da tasiri a kan daban-daban pathological zagi kamar cerebral ischemia, hypoxia, rauni, kuma neurodegeneration.
An yarda da shi a cikin Rasha a matsayin ƙarin magani don m bugun jini, raunin kwakwalwa mai rauni, da matakin farko Cutar Parkinson.
a takaice, NA Semax Amidate yana amfani da gyare-gyaren sinadarai don shawo kan iyakokin peptide na halitta, ta haka ya zarce na al'ada Semax in haɓakar fahimi, neuroprotection, yanayin yanayi, da gyara rauni.
Wannan yana da mahimmancin mahimmancin asibiti don maganin cututtuka na neurodegenerative da kuma inganta tsarin kulawa na tsakiya na aikin farfadowa.
Jeri
AC-met-glu-his-phe-pro-gly-pro-nh2
Lambar CAS
/
Tsarin kwayoyin halitta
Saukewa: C39H54N10O10S
Nauyin Kwayoyin Halitta
854.98
Binciken NA Semax Amidate
NA Semax Amidate yana nuna inganci kwatankwacin na gargajiya anxiolytic kwayoyi a da yawa preclinical model.
1.Haɓaka Fahimta da Ƙarfin Jijiya
NA Semax Amidate yana kunna fasalin rubutun CREB, upregulating BDNF Maganar kwayoyin halitta da haɓaka matakan BDNF neuronal ta sama 40%.
Wannan kuma yana inganta dendritic kashin baya samuwar, jagorar axonal, da haɗuwa da furotin mai yawa na postsynaptik 95 (Saukewa: PSD-95), don haka inganta iyawar koyo.
Gwaje-gwajen kwaikwaiyon halittu sun nuna a 35-50% haɓakawa a cikin ƙimar riƙe ƙwaƙwalwar ajiya a cikin mahallin mahallin yanayin tsoro gwaje-gwaje.
Yanke kwakwalwa electrophysiological rikodi sun tabbatar da karuwa LTP amplitude da duration, yana nuna cewa NA Semax Amidate yana sake fasalin synaptic filastik bakin kofa ta hanyar zurfafa kunnawa neurotrophic factor hanyar sadarwa.
2.Kariyar Neuro da Gyara
NA Semax Amidate yana kunna adenylate cyclase (AC)-Hanyar cAMP-PKA don daidaitawa mitochondrial yiwuwar membrane, ya hana cytochrome C saki, kuma yana dannewa kaso-3 cascade kunnawa, ta haka toshe lokacin kisa na apoptosis.
A lokaci guda, yana ingantawa superoxide dismutase magana da kuma hana wuce kima kumburi cytokine samarwa.
A cikin bera tsakiyar cerebral artery occlusion model, ya rage ciwon kwakwalwa girma ta wuce 50%.
A cikin wani MPTP samfurin cutar Parkinson, ya karu dopaminergic neuron tsira ta 35%, nuna m neuroprotection.
3.Tasirin Anxiolytic da Analgesic
NA Semax Amidate yana haɓaka alaƙa ga endogenous enkephalins kuma β-endorphin yayin hanawa G protein-haɗe-haɗe receptor kinase (GIRKI)-shiga tsakani mai karɓa na ciki da rashin jin daɗi, ta haka tsawaitawa analgesic sigina.
Har ila yau, yana rage yawan jin zafi mai zafi na FTO.
A cikin samfurin linzamin kwamfuta, bakin zafi aka daukaka ta 30-40% kuma ya kasance dagagge ga 4 ku 6 hours.
A cikin rauni na maƙarƙashiya (CCI) samfura, inji allodynia aka rage ta 50%, kara tabbatar da NA Semax Amidate bayyanannen anti-danniya da kaddarorin daidaita yanayi.
NA Semax Amidate yana nuna inganci kwatankwacin magungunan anxiolytic na gargajiya a cikin nau'ikan madaidaicin tsari da yawa..
4.Haɓaka Fahimta da Ƙarfin Jijiya
NA Semax Amidate yana kunna yanayin rubutun CREB, haɓaka maganganun kwayoyin BDNF da haɓaka matakan BDNF neuronal ta sama 40%.
Wannan kuma yana inganta samuwar kashin baya na dendritic, jagorar axonal, da haɗuwa da furotin mai yawa na postsynaptik 95 (Saukewa: PSD-95), don haka inganta iyawar koyo.
Gwaje-gwajen kwaikwaiyon halittu sun nuna a 35-50% haɓaka ƙimar riƙe ƙwaƙwalwar ajiya a cikin gwaje-gwajen yanayin tsoro na mahallin.
Rakodin yanki na kwakwalwa na electrophysiological yana tabbatar da ƙara girman LTP da tsawon lokaci, yana nuna cewa NA Semax Amidate yana sake fasalin ƙofofin synaptic filastik ta hanyar haɓakar hanyar sadarwa ta hanyar neurotrophic..
5.Kariyar Neuro da Gyara
NA Semax Amidate yana kunna adenylate cyclase (AC)-Hanyar cAMP-PKA don daidaita yuwuwar mitochondrial membrane, yana hana sakin cytochrome C, kuma yana hana caspase-3 kunnawar cascade, don haka toshe lokacin aiwatar da apoptosis.
A lokaci guda, yana haɓaka maganganun superoxide dismutase kuma yana hana haɓakar cytokine mai kumburi da yawa.
A cikin ƙirar bera ta tsakiya ta rufe jijiya, ya rage karfin ciwon kwakwalwa ta fiye da haka 50%.
A cikin tsarin MPTP na cutar Parkinson, ya ƙãra dopaminergic neuron rayuwa ta 35%, nuna m neuroprotection.
6.Tasirin Anxiolytic da Analgesic
NA Semax Amidate yana haɓaka alaƙa ga enkephalins na endogenous da β-endorphin yayin da ke hana G protein-coupled receptor kinase (GIRKI)-shiga tsakani mai karɓa na ciki da rashin jin daɗi, don haka tsawaita siginar analgesic.
Har ila yau, yana rage yawan jin zafi mai zafi na FTO.
A cikin samfurin linzamin kwamfuta, zafi ƙofofin da aka dagawa ta 30-40% kuma ya kasance dagagge ga 4 ku 6 hours.
A cikin rauni na maƙarƙashiya (CCI) samfura, inji allodynia ya rage ta 50%, kara tabbatar da NA Semax Amidate bayyanannen anti-danniya da kaddarorin daidaita yanayi.
COA
HPLC
MS
