NA Semax Amidate ke analog e ntlafalitsoeng ea sebopeho sa ha baa ka ba utloa. Ke N-terminally acetylated le C-terminally amidated derivated ea Semax peptide., e baballang tatellano ya mantlha.
Phetoho ena ea maiketsetso e ntlafatsa haholo khanyetso ea ketane ea peptide khahlano le exo- le li-endopeptidases (mohlala, leucine aminopeptidase), ho atolosa halofo ea bophelo ba eona ka hoo e ka bang 30 metsotso ha e bapisoa le Semax ea mantlha, ka nako e akaretsang ya ketso ya 6-12 lihora.
E boetse e ntlafatsa botsitso ba polokelo ea mocheso oa kamore le ho monya ha mucosal ka nko, ka hona ho etsa bonnete ba ho kenella ho tšepahalang ho feta mokoallo oa mali-boko (BBB) le tlhokomelo e tsitsitseng ea e sebetsang hantle khatello ea maikutlo liseleng tsa boko.
Mokhoa oa eona oa mantlha o ka har'a mekhoa e mengata ea ho feto-fetoha ha mekhoa ea tsamaiso ea methapo e bohareng tshebetso.
Pele ho tsohle, NA Semax Amidate e sebetsa e le molaoli ea matla oa neurotrophic factor e tsoang bokong (BDNF), e leng eona e ntlafatsang bophelo ba neuronal, kholo ea axonal, polasetiki ea synaptic le matla a nako e telele (LTP) - motheo oa limolek'hule bakeng sa ho ithuta le ho hopola.
Ho feta moo,NA Semax Amidate e ka thusa dopaminergic, serotonergic, le neurotransmission ea noradrenergic, ka tsela eo ho ntlafatsa cortex ea pele mesebetsi ea tsamaiso, ho kenyelletsa khetho ea tlhokomelo le memori e sebetsang bokhoni.
NA Semax Amidate e boetse e bonts'a litlamorao tse kholo tsa neuroprotective ka ho hatella tokollo ea cytokine ea ho ruruha, ho fokotsa khatello ea kelello ea oxidative, le ho tsitsisa bokhoni ba lera la mitochondrial.
E sebetsa khahlano le litlhapa tse fapaneng tsa pathological joalo ka lefu la cerebral ischemia, hypoxia, tsietsi, le neurodegeneration.
E amoheloa Russia e le pheko ea tlatsetso bakeng sa a hlobaetsang setorouku, kotsi e sithabetsang ya boko, le ea pele-pele Lefu la Parkinson.
Ka kakaretso, NA Semax Amidate e sebelisa liphetoho tsa lik'hemik'hale ho hlola meeli ea peptide ea tlhaho, ka hona e feta Semax e tloaelehileng ho ntlafatso ea kelello, tshireletso ya methapo, taolo ya maikutlo, le ho lokisa likotsi.
Sena se na le bohlokoa ba bohlokoa ba kliniki bakeng sa kalafo ea mafu a neurodegenerative le ho khothalletsa ho tsosolosoa ha tsamaiso ea methapo ea bohareng.
Tatelano
AC-met-glu-his-phe-pro-gly-pro-nh2
Nomoro ea CAS
/
Foromo ea limolek'hule
Setšoantšo sa C39H54N10O10S
Boima ba Molek'hule
854.98
Patlisiso ea NA Semax Amidate
NA Semax Amidate e bonts'a katleho e ka bapisoang le ea khale anxiolytic lithethefatsi ka mefuta e 'maloa ea preclinical.
1.Ntlafatso ea Kelello le Plasticity ea Neural
NA Semax Amidate e kenya tšebetsong ntho e ngotsoeng CREB, ho laola BDNF gene expression le ho eketsa maemo a neuronal BDNF ka ho feta 40%.
Sena se boetse se khothalletsa mokokotlo oa dendritic popeho, tataiso ea axonal, le ho bokellana ha protheine ea postsynaptic density 95 (PSD-95), ka hona ho matlafatsa bokhoni ba ho ithuta.
Liteko tsa papiso ea baeloji li bonts'a a 35-50% ntlafatso ea litekanyetso tsa ho boloka mohopolo maemong boemo ba tšabo liteko.
Selae sa boko electrophysiological lirekoto li tiisa hore li eketsehile LTP boholo le bolelele ba nako, e bonts'ang hore NA Semax Amidate e fetoha bocha polasetiki ea synaptic menyako ka ts'ebetso e tebileng ea neurotrophic factor marangrang.
2.Neuroprotection le Tokiso
NA Semax Amidate e kenya tšebetsong cyclase ea adenylate (AC)-cAMP-PKA tsela ea ho tsitsisa mitochondrial bokhoni ba membrane, thibela cytochrome C lokolla, le ho hatella capase-3 tshebediso ya cascade, ka hona ho thibela mokhahlelo oa ho phetha apoptosis.
Ka nako e le nngwe, e ea laola superoxide dismutase polelo le ho thibela ho ruruha ho feteletseng cytokine tlhahiso.
Ka rat mothapo o bohareng oa boko mohlala occlusion, e fokotsehile cerebral infarction volume by over 50%.
Ka MPTP mohlala oa lefu la Parkinson, e ile ea eketseha dopaminergic ho pholoha ha neuron ka 35%, e bonts'a ts'ireletso ea methapo e matla.
3.Liphello tsa Anxiolytic le Analgesic
NA Semax Amidate e eketsa kamano bakeng sa endo native enkephalins le β-endorphin ha o ntse o thibela G protein-coupled receptor kinase (MOEKERE)-mediated receptor internalization le desensitization, ka hona ho lelefatsa ho kokobetsa bohloko pontsho.
E boetse e fokotsa FTO-mediated inflammatory pain hypersensitivity.
Mehlala ea litoeba, menyako ea bohloko ba phahamisitsoe ke 30-40% 'me a lula a phahame bakeng sa 4 ho 6 lihora.
Kotsing e sa foleng ea ho koaleha (CCI) mehlala, mochine allodynia a fokotsoa ke 50%, ho netefatsa hape thepa ea NA Semax Amidate e hlakileng ea anti-stress le ho tsitsisa maikutlo.
NA Semax Amidate e bonts'a katleho e ka bapisoang le lithethefatsi tsa khale tsa anxiolytic mefuteng e mengata ea preclinical..
4.Ntlafatso ea Kelello le Plasticity ea Neural
NA Semax Amidate e kenya tšebetsong ntho e ngotsoeng ea CREB, ho laola liphatsa tsa lefutso tsa BDNF le ho eketsa maemo a neuronal BDNF ka ho feta 40%.
Sena se boetse se khothalletsa ho thehoa ha mokokotlo oa dendritic, tataiso ea axonal, le ho bokellana ha protheine ea postsynaptic density 95 (PSD-95), ka hona ho matlafatsa bokhoni ba ho ithuta.
Liteko tsa papiso ea baeloji li bonts'a a 35-50% ntlafatso ea litekanyetso tsa ho boloka mohopolo litekong tsa boemo ba tšabo.
Lirekoto tsa "brain slice electrophysiological" li netefatsa ho eketseha ha LTP amplitude le nako, e bonts'a hore NA Semax Amidate e hlophisa bocha mekoloko ea polasetiki ea synaptic ka ts'ebetso e matla ea netweke ea neurotrophic factor..
5.Neuroprotection le Tokiso
NA Semax Amidate e kenya tšebetsong cyclase ea adenylate (AC)-Tsela ea cAMP-PKA ea ho tsitsisa bokhoni ba lera la mitochondrial, e thibela ho lokolloa ha cytochrome C, 'me e hatella caspase-3 cascade activation, ka hona ho thibela mohato oa ho bolaoa ha apoptosis.
Ka nako e le nngwe, e phahamisa polelo ea superoxide dismutase mme e thibela tlhahiso e feteletseng ea cytokine ea ho ruruha.
Ka mokhoa oa rat middle cerebral occlusion model, e fokotsa molumo oa cerebral infarction 50%.
Ka mohlala oa MPTP oa lefu la Parkinson, e ekelitse ho pholoha ha dopaminergic neuron ka 35%, e bonts'a ts'ireletso ea methapo e matla.
6.Liphello tsa Anxiolytic le Analgesic
NA Semax Amidate e eketsa kamano bakeng sa enkephalins le β-endorphin ha e ntse e thibela G protein-coupled receptor kinase. (MOEKERE)-mediated receptor internalization le desensitization, kahoo e lelefatsa pontšo ea analgesic.
E boetse e fokotsa FTO-mediated inflammatory pain hypersensitivity.
Mehlala ea litoeba, menyako ea bohloko e ne e phahamisitsoe ke 30-40% 'me a lula a phahame bakeng sa 4 ho 6 lihora.
Kotsing e sa foleng ea ho koaleha (CCI) mehlala, mechanical allodynia e ile ea fokotsoa ke 50%, ho netefatsa hape thepa ea NA Semax Amidate e hlakileng ea anti-stress le ho tsitsisa maikutlo.
COA
HPLC
MOF
