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 mwepụta 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% improvement in memory retention rates in contextual fear conditioning ule.
Brain slice electrophysiological recordings confirm increased LTP amplitude and duration, indicating that NA Semax Amidate reshapes synaptik plasticity thresholds through profound activation of the ihe na-akpata neurotrophic netwọk.
2.Neuroprotection and Repair
NA Semax Amidate activates the adenylate cyclase (AC)-cAMP-PKA pathway to stabilize mitochondrial membrane potential, inhibits cytochrome C ntọhapụ, and suppresses caspase-3 cascade activation, thereby blocking the execution phase of apoptosis.
Concurrently, it upregulates superoxide dismutase expression and inhibits excessive inflammatory cytokine mmepụta.
In a rat middle cerebral artery occlusion model, it reduced cerebral infarction volume by over 50%.
In an MPTP model of Parkinson’s disease, it increased dopaminergic neuron survival by 35%, demonstrating potent neuroprotection.
3.Anxiolytic and Analgesic Effects
NA Semax Amidate increases affinity for 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 site 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 ndochi egwu ọnọdụ.
Ndekọ eletrọjiji akụkụ ụbụrụ na-egosi 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 and Repair
NA Semax Amidate activates the 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.
Concurrently, ọ na-akwalite okwu superoxide dismutase ma na-egbochi mmepụta cytokine na-akpasu oke iwe.
N'ime ihe nkpuchi oghere nke etiti ụbụrụ oke oke, ọ belatara olu infarction ụbụrụ site n'ifefe 50%.
N'ụdị MPTP nke ọrịa Parkinson, ọ mụbara dopaminergic neuron nlanarị site 35%, demonstrating potent neuroprotection.
6.Anxiolytic and Analgesic Effects
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
