Adalank bụ peptide synthetic analogue nke selank, na mgbanwe kemịkalụ ezubere iche.
A haziri peptide dị ka a ewepụtara nke nootropic ọgwụ Selank, yana mgbakwunye nke ọrụ N-terminal acetylated nke na-eme ka nhazi ya dị ka adamantane na-egbochi ya..
Mgbanwe a na-arụ ọrụ dị ka onye ike synergistic siri ike nke anxiolytic – nootropic compound - Selank.
Ọ gafere ndị ogbenye Selank mgbochi ụbụrụ ọbara (BBB) ntinye, si otú ahụ na-abawanye Central ụjọ usoro ọrụ-Adalank nke ukwuu.
Mgbakwunye nke ihe otu acetyl na-ewepụ ụgwọ dị mma nke otu amino free N-terminal ma belata ụgwọ net nke peptide..
Nke a physicochemical mmezi na-ebuli ihe ebe isoelectric na elu Njirimara nke Adalank, ibelata mmekọrịta electrostatic na-abụghị nke akọwapụtara.
N'ihi ya, molecule ọgwụ na-agafe ihe mgbochi ụbụrụ ọbara-n'ụzọ dị mfe ma rute na sistemụ ụjọ..
Ọzọkwa, acetylation na-echebe Adalank si Exopeptidase nbibi na-abawanye nke ọma na vivo ọkara ndụ ya.
Nke a na-enye uru dị n'ọkwa ọbara ọgwụgwọ ogologo oge - ma na-ebelata doses ugboro ugboro.
Ntinye nke adamantane na-emepụta “isi conformation” kwụsiri ike n'ime peptide Adalank.
Nke a na-enye nghazi oghere na peptide linear na-agbanwe na mbụ, na-akwalite stereochemical conformation dị mkpa maka ihe omume ndu ọbụna na ya enweghị oke ala.
Nke a na-eme ka ike Adalank gafere ihe mgbochi ụbụrụ ọbara.
Na mgbakwunye, Adalank na-egosipụta ụfọdụ mmetụta immunomodulatory.
Usoro
ac-thr-lys-pro-arg-pro-gly-pro-Adamantane-nh2
Nọmba CAS
/
Usoro ihe omimi
C46H75N13O10
Ibu molekụla
970.19
Nnyocha nke Adalank:
1.Usoro nke Omume
Ịrụ ọrụ-maara ihe, Ọdịdị siri ike nke Adalank dabara na nke ahụ allosteric modulation saịtị nke GABA_A nnata subunit alfa, na-enye ike anxiolytic mmetụta.
Ọzọkwa, moiety adamantane na-enyere aka mmekọrịta hydrophobic na NMDA nnata Mpaghara ọwa iji mee ka mgbaba calcium na-agafe agafe ma chebe megide mmerụ ahụ excitotoxic.
Ihe onwunwe a nwere ikike neuroprotection na ụdị nke ischemic ụbụrụ mmerụ na nsogbu nrụgide post-traumatic (PTSD).
2.Mmetụta Anxiolytic
Dị ka ihe nrụpụta kachasị nke Selank, Adalank na-ejigide mmekọrịta dị elu na saịtị benzodiazepine na GABA_A receptor α-subunit..
Agbanyeghị, N-terminal acetylation na adamantane scaffold gbanwere usoro njikọ ahụ site na "mgbanwe". kpaliri dabara"na" n'ọdụ ụgbọ mmiri siri ike ".
Nke a na-akwalite neurotransmission GABAergic inhibitory, na-akwalite ntinye chloride na mbelata ọrụ ngwa ngwa na sekit akwara amygdala-prefrontal cortex..
N'adịghị ka benzodiazepines, Adalank na-egosi ụdị nhọrọ nnabata dị elu, na-eme ka mmetụta anxiolytic na-adịgide adịgide na-enweghị nkwụsịtụ, izu ike akwara, ma ọ bụ ike riri ahụ metụtara ọgwụ ọdịnala.
Ya ọgwụgwọ index bụ 3 ka 5 ugboro obosara, na-akwado njikwa ogologo oge nke nsogbu nchekasị zuru oke na nsogbu nchegbu ọnọdụ.
3.Mmelite ọgụgụ isi na nkwalite ebe nchekwa
Adalank na-egbochi ọrụ nke ụzọ mkpali NF-κB nke ọma ma na-abawanye BDNF mRNA okwu site 50%-80% n'ime hippocampus.
Nke a na-eduga na ịgbalite-nke mgbada Akt/CREB ụzọ mgbaàmà, na-eme ka ntinye na mmezi LTP aka.
Ọ na-eme ka njide ebe nchekwa dịkwuo mma ngafe ezere ule, na-eme ka mmụta gbasara ohere dị n'ime Morris mmiri maze, na-emegide scopolamine-kpatara mmebi cholinergic.
Data izizi na-egosi na Adalank na-ebelata mperi ebe nchekwa ọrụ site na 40%-60% ma na-ebelata ikike ncheta eke eke na ụmụ anụmanụ merela agadi, na-atụ aro itinye aka na nsogbu mmụta, obere nghọta mmebi, yana mbelata ebe nchekwa metụtara afọ.
4.Mmetụta Neuroprotective
Ọdịdị adamantane na Adalank na-eṅomi omume nke memantine, na-eme ihe dị ka onye na-adịghị asọmpi NMDA nnata antagonist nke na-eme ka mgbochi voltaji dabere na ọwa mepere emepe yana ụkpụrụ physiological nke ntinye calcium.
Ọ na-ebelata nnabata nke ca²⁺ site na 60-70% na-enweghị mmebi nke synapti ca²⁺ physiological., imezu profaịlụ neuroprotective ahọpụtara na-emebighị ọrụ nkịtị.
Ya mere, Ọmụmụ ihe izizi na-akọwapụta ikike ntụgharị asụsụ Adalank nwere maka itinye aka n'oge na nnukwu ọrịa strok, ọkpụkpụ azụ azụ, na ọrịa neurodegenerative.
COA
HPLC
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