Ko Adalank he peptide tairitenga o kirikiri, me te whakarereketanga matū.
Ko te peptide i hangaia hei a pärönaki o nga nootropic tarukino Selank, me te taapiri o te mahi acetylated N-terminal e whakarei ake ana i tana hanganga-a-amantane-rite-sterically-constraining.
Ko tenei whakarereketanga ka mahi hei potentiator synergistic kaha o te anxiolytic – pūhui nootropic Selank.
Ka huri i nga rawakore a Selank arai toto-roro (BBB) urunga, na reira ka piki ake te pūnaha io pokapū mahi o Adalank tino.
Ko te taapiri o te roopu acetyl ka whakakore i te utu pai o te roopu amino kore-waa-N ka whakaheke i te utu kupenga o te peptide.
Ko tenei whakatikatika matū ahupūngao e arotau ana i te ira hauhiko me nga ahuatanga mata o Adalank, te whakaiti i nga taunekeneke hiko kore-motuhake.
Ko te mutunga, the drug molecule crosses the blood–brain barrier more easily and reaches the central nervous system.
I tua atu, whakakaha protects Adalank from exopeptidase degradation and significantly increases its in vivo half-life.
This provides the advantage of prolonged therapeutic blood levels and reduces frequent dosing.
The inclusion of adamantane creates a stable “conformation core” in the Adalank peptide.
This imparts a fixed spatial orientation to the initially flexible linear peptide, promoting the stereochemical conformation necessary for biological activity even in its unbound state.
This greatly improves Adalank’s ability to cross the blood-brain barrier.
I tua atu, Adalank exhibits certain immunomodulatory effects.
Raupapa
ac-thr-lys-pro-arg-pro-gly-pro-Adamantane-nh2
Tau CAS
/
Tātai rāpoi
C46H75N13O10
Taumaha rāpoi
970.19
Research Of Adalank:
1.Mechanism of Action
Te kaha-whakaaro, Ko te hanganga maro o Adalank e tino rite ana ki te whakarerekētanga allosteric pae o te GABA_A kaiwhiwhi wae iti alpha, kaha ake te tuku anxiolytic pānga.
I tua atu, ka taea e te moiety adamantane te taunekeneke hydrophobic i roto i te Kaiwhiwhi NMDA te waahi hongere ki te whakaheke i te urunga o te konupūmā me te tiaki i te whara excitotoxic.
Kei tenei rawa te kaha mo neuroprotection i roto i nga tauira o te whara roro ischemic me te raruraru i muri i te mamae (PTSD).
2.Pānga Anxiolytic
Ka rite ki te pärönaki papaitia o Selank, Ka mau tonu a Adalank i te hononga hononga-nui ki te pae benzodiazepine i runga i te GABA_A receptor α-subunit.
Heoi ano, ka huri te acetylation N-terminal me te scaffold adamantane i te aratau here mai i te “ngawari uru whakaawe” ki te “taupu tika”.
Ma tenei ka whakarei ake i te neurotransmission aukati GABAergic, te whakatairanga i te urunga pūhaumāota me te whakaheke tere o te ngohe i roto i nga hikoi neural amygdala-prefrontal cortex hyperactive.
He rereke ki te benzodiazepines, E whakaatu ana a Adalank i te tohu-a-te-nui-a-tangata momo iti, te whakaahei i nga paanga anxiolytic toi tonu me te kore o te whakarokiroki, whakangā uaua, he waranga ranei e pa ana ki nga rongoa tuku iho.
Ko ona tohu rongoa ko 3 ki 5 wa whanui, te tautoko i te whakahaeretanga mo te wa roa whakararuraru ohorere me nga raruraru ohorere.
3.Te Whakanui Hinengaro me te Maharahara
Ka kaha te aukati a Adalank i te whakahohenga o te ara inflammatory NF-κB me te piki haere BDNF mRNA whakapuaki na 50%-80% i roto i te hippocampus.
Ko tenei ka arai atu ki te whakahohenga o te awaawa Akt/CREB nga huarahi tohu, te whakahaere i te whakauru me te tiaki LTP.
Ka tino whakapai ake te pupuri mahara ki roto te karo hāngū whakamātautau, whakarei ake i te ako mokowhiti i roto i te Maze wai Morris, me te whakakeke scopolamine-te kino cholinergic.
Ko nga raraunga preclinical e tohu ana ka whakaitihia e Adalank nga hapa mahara mahi na 40%-60% me te whakaiti i te heke o te mahara maori ki nga kararehe tawhito, e whakaatu ana i te whakamahinga mo nga mate ako, te ngoikoretanga o te hinengaro ngawari, me te hekenga mahara e pa ana ki te reanga.
4.Nga Painga Neuroprotective
Ko te hanganga adamantane i Adalank e whai ana i te mahi a memantine, te mahi hei whakataetae kore Kaiwhiwhi NMDA he kaitukino e pa ana ki te aukati ngaohiko-whakawhirinaki o nga hongere tuwhera me te ture whaiaroaro o te urunga o te konupūmā.
Ka whakahekehia te urunga pathological Ca²⁺ mā te 60–70% me te kore e whakararu i te tohu tohu Ca²⁺ tinana., te whakatutuki i tetahi tohu neuroprotective whiriwhiri me te kore e pakaru te mahi noa.
Koia, Ko nga rangahau preclinical e whakaatu ana i te kaha whakamaoritanga nui o Adalank mo te wawaotanga moata mo te whiu mate, te whara o te taurakira, a nga mate neurodegenerative.
COA
HPLC
MS
