NA Semax Amidate bụ analọgụ ahaziri nhazi nke anụghị. Ọ bụ N-terminally acetylated na C-terminally amidated ewepụtara nke Semax peptide., nke na-echekwa usoro isi.
Mgbanwe a rụrụ arụ na-eme ka nguzogide nke yinye peptide megide exo- na endopeptidases (dịka ọmụmaatụ leucine aminopeptidase), ịgbatị ọkara ndụ ya ihe dị ka 30 nkeji tụnyere nke mbụ Semax, na ngụkọta oge nke edinam nke 6-12 awa.
Ọ na-akwalitekwa nkwụsi ike nchekwa okpomọkụ na ime mucosal imi, si otú huu ọzọ a pụrụ ịdabere na penetration nke ihe mgbochi ụbụrụ ọbara (BBB) na nkwado na-adịgide adịgide nke dị irè ntinye uche gradient na ụbụrụ anụ ahụ.
Isi ya usoro dabere na multi-ụzọ modulation nke Central ụjọ usoro ọrụ.
Nke mbụ na nke mbụ, NA Semax Amidate na-arụ ọrụ dị ka onye na-achịkwa ike nke ihe neurotrophic sitere n'ụbụrụ (BDNF), nke na-eme ka ndụ neuronal dịkwuo mma, uto axonal, synaptik plasticity na ike ogologo oge (LTP) - ntọala molekụla maka mmụta na ebe nchekwa.
Ọzọkwa,NA Semax Amidate na-akwalite dopaminergic, serotonergic, na noradrenergic neurotransmission, si otú na-ebuli elu prefrontal cortex Executive ọrụ, gụnyere nlebara anya selectivity na ebe nchekwa na-arụ ọrụ ikike.
NA Semax Amidate na-egosipụtakwa mmetụta neuroprotective dị ịrịba ama site na ibelata ntọhapụ cytokine mkpali., ibelata mmebi nrụgide oxidative, na ime ka akpụkpọ ahụ mitochondrial guzosie ike.
Ọ dị irè megide mkparị pathological dị iche iche dị ka cerebral ischemia, hypoxia, trauma, na neurodegeneration.
A kwadoro ya na Russia ka ọ bụrụ ọgwụgwọ mgbakwunye maka nnukwu ọrịa strok, mmerụ ụbụrụ traumatic, na mmalite-ogbo Ọrịa Parkinson.
Na nchịkọta, NA Semax Amidate na-eji mgbanwe kemịkalụ iji merie oke nke peptide eke, si otú a gafere Semax omenala na nkwalite ọgụgụ isi, neuroprotection, ụkpụrụ ọnọdụ, na mmezi mmerụ ahụ.
Nke a na-ejide ịrịba Clinical mkpa maka ọgwụgwọ nke ọrịa neurodegenerative na nkwalite nke usoro nhụjuanya nke etiti na-arụ ọrụ mgbake.
Usoro
AC-met-glu-his-phe-pro-gly-pro-nh2
Nọmba CAS
/
Usoro ihe omimi
C39H54N10O10S
Ibu molekụla
854.98
Nnyocha nke NA Semax Amidate
NA Semax Amidate na-egosipụta ịdị irè ya na oge gboo anxiolytic ọgwụ na ọtụtụ preclinical ụdị.
1.Nkwalite ọgụgụ isi na Plasticity Neural
NA Semax Amidate na-arụ ọrụ ihe odide ederede CREB, na-akwalite BDNF okwu mkpụrụ ndụ ihe nketa na ịbawanye ọkwa BDNF neuronal site n'ifefe 40%.
Nke a n'aka na-akwalite spine dendritic nhazi, nduzi axonal, na mkpokọta protein njupụta postsynaptik 95 (PSD-95), si otú a na-akwalite ikike mmụta.
Nnwale ịme anwansị ndu na-egosi a 35-50% mmelite na ọnụego njide ebe nchekwa na onodu oyi oyi ule.
Iberibe ụbụrụ electrophysiological Ndekọ abawanyela LTP njupụta na ogologo oge, na-egosi na NA Semax Amidate na-emegharị synaptik plasticity ọnụ ụzọ site na ịgbalite nke ọma ihe na-akpata neurotrophic netwọk.
2.Neuroprotection na Mmezi
NA Semax Amidate na-arụ ọrụ adenylate cyclase (AC)-Ụzọ cAMP-PKA iji kwụsie ike mitochondrial ikike nke akpụkpọ ahụ, na-egbochi cytochrome C ntọhapụ, na-egbochikwa agba -3 ịgbalite cascade, si otú igbochi igbu oge nke apoptosis.
N'otu oge, ọ na-akwalite superoxide dismutase nkwupụta ma na-egbochi oke mkpali cytokine mmepụta.
Na oke etiti cerebral akwara ụdị occlusion, o belatara ọrịa ụbụrụ ụbụrụ olu site n'ofe 50%.
N'ime otu MPTP ụdị ọrịa Parkinson, ọ mụbara dopaminergic neuron lanarị site 35%, na-egosipụta ike neuroprotection.
3.Mmetụta anxiolytic na analgesic
NA Semax Amidate na-abawanye mmekọrịta maka endogenous enkephalins na β-endorphin mgbe inhibit G kinase nnabata protein jikọtara ọnụ (GIRIK)-internation nnabata na desensitization mediated, si otú a na-agbatịkwu oge analgesic na-egosi.
Ọ na-ebelatakwa ihe mgbu hypersensitivity na FTO-mediated.
Na ụdị òké, ọnụ ụzọ mgbu e buliri site 30-40% wee nọgide na-ebuli elu maka 4 ka 6 awa.
Na-adịghị ala ala constriction mmerụ (CCI) ụdị, n'ibu allodynia e belatara ya 50%, na-akwadokwa NA Semax Amidate doro anya mgbochi nchekasị na ihe na-eme ka ọnọdụ obi sie ike.
NA Semax Amidate na-egosiputa ịdị irè ya na ọgwụ anxiolytic oge gboo n'ọtụtụ ụdị preclinical..
4.Nkwalite ọgụgụ isi na Plasticity Neural
NA Semax Amidate na-arụ ọrụ ihe odide ederede CREB, na-akwalite okwu mkpụrụ ndụ BDNF yana ịba ụba ọkwa BDNF neuronal site na ihe karịrị 40%.
Nke a na-akwalite nguzobe spine dendritic, nduzi axonal, na mkpokọta protein njupụta postsynaptik 95 (PSD-95), si otú a na-akwalite ikike mmụta.
Nnwale ịme anwansị ndu na-egosi a 35-50% mmụba n'ọnụego njide ebe nchekwa n'ule ọnọdụ egwu ọnọdụ.
Ndekọ elektrọnijiji akụkụ ụbụrụ na-akwado mmụba LTP na ogologo oge, na-egosi na NA Semax Amidate na-emezigharị ọnụ ụzọ synaptic plasticity site na ntinye miri emi nke netwọkụ ihe na-akpata neurotrophic..
5.Neuroprotection na Mmezi
NA Semax Amidate na-arụ ọrụ adenylate cyclase (AC)-Ụzọ cAMP-PKA iji mee ka akpụkpọ ahụ mitochondrial kwụsie ike, na-egbochi mwepụta cytochrome C, ma na-egbochi ịgbalite caspase-3 cascade, si otú ahụ na-egbochi oge igbu nke apoptosis.
N'otu oge, ọ na-akwalite okwu superoxide dismutase ma na-egbochi mmepụta cytokine na-akpasu oke iwe.
N'ime ụdị mgbachi akwara nke etiti oke oke, ọ belatara olu infarction ụbụrụ site n'ifefe 50%.
Na ụdị MPTP nke ọrịa Parkinson, ọ mụbara nlanarị neuron dopaminergic site na 35%, na-egosipụta ike neuroprotection.
6.Mmetụta anxiolytic na analgesic
NA Semax Amidate na-abawanye mmekọrịta maka enkephalins endogenous na β-endorphin ka ọ na-egbochi G protein-coupled receptor kinase (GIRIK)-internation nnabata na desensitization mediated, si otú ahụ na-agbatị mgbaàmà analgesic.
Ọ na-ebelatakwa ihe mgbu hypersensitivity na FTO-mediated.
Na ụdị òké, Ebuliri ọnụ ụzọ mgbu site na 30-40% wee nọgide na-ebuli elu maka 4 ka 6 awa.
Na-adịghị ala ala constriction mmerụ (CCI) ụdị, Mechanical allodynia e belatara site na 50%, na-akwadokwa NA Semax Amidate doro anya mgbochi nchekasị na ihe na-eme ka ọnọdụ obi sie ike.
COA
HPLC
MS
