Selank hmoov, molecular formula C33H57N11O9, CAS 129954-34-3. Feem ntau yog dawb los yog tawm dawb crystalline hmoov, tsis muaj ntxhiab los yog yuav luag tsis muaj ntxhiab, nrog rau qee qhov kev ruaj ntseg, tab sis yuav degrade nyob rau hauv qhov kub thiab txias, high humidity, muaj zog lub teeb thiab lwm yam kev mob. Nws solubility sib txawv nyob ntawm qhov hnyav, thiab nws feem ntau yog soluble hauv cov kuab tshuaj polar piv txwv li dej thiab physiological saline. Nws tau pib tsim los ntawm kev tshawb fawb ntawm Tuftsin, peptide uas txhawb nqa phagocytosis. Peptides uas txhawb phagocytosis muaj peev xwm txhim kho phagocytic kev ua haujlwm ntawm lub cev tiv thaiv kab mob, tab sis lawv muaj qhov tsis zoo xws li kev ruaj ntseg tsis zoo thiab lub neej luv luv. Cov kws tshawb fawb tau tsim cov khoom los ntawm kev hloov kho thiab hloov kho nws cov qauv. Tom qab kev tshawb nrhiav kev tshawb fawb dav dav, nws tau pom tias nws tsis tsuas yog khaws qee lub cev tiv thaiv kab mob, tab sis kuj tseem muaj cov tshuaj pharmacological tshwj xeeb xws li kev tiv thaiv kev ntxhov siab thiab kev paub txog kev txhim kho. Nrog rau qhov tob ntawm kev tshawb nrhiav, nws tau ua rau hauv cov hmoov hmoov rau kev yooj yim ntawm kev khaws cia, kev thauj mus los, thiab kev siv.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
Peb Cov Khoom
Selank +. COA
Pharmacological kev ua
Neurotransmitter tswj mechanism:
Selank hmoovtuaj yeem tswj hwm ntau yam kab mob neurotransmitter hauv lub hauv paus paj hlwb. Nws tuaj yeem ua rau kev tso tawm thiab kev ua haujlwm ntawm gamma aminobutyric acid (GABA), ib qho tseem ceeb inhibitory neurotransmitter nyob rau hauv lub hauv paus paj hlwb sytem uas yuav suppress neuronal overexcitation thiab alleviate anxiety cov tsos mob. Nyob rau tib lub sijhawm, nws tseem tuaj yeem tswj hwm cov kab ke serotonin (5-HT), nce qhov concentration ntawm serotonin hauv synaptic cleft. Serotonin muaj feem cuam tshuam nrog kev tswj hwm kev xav, thiab nws cov theem tsis sib xws tuaj yeem ua rau muaj kev xav tsis zoo xws li kev ntxhov siab thiab kev nyuaj siab. Tsis tas li ntawd, nws kuj tseem tuaj yeem cuam tshuam rau cov metabolism thiab kev sib kis ntawm lwm cov neurotransmitters piv txwv li dopamine thiab norepinephrine, ua kom tswj tau qhov excitability ntawm lub paj hlwb thiab tawm tsam kev ntxhov siab.
Kev tswj hwm neuroendocrine:
Cov xeev ntxhov siab feem ntau nrog kev cuam tshuam hauv cov kab mob neuroendocrine, piv txwv li kev ua kom ntau dhau ntawm hypothalamic pituitary adrenal axis (HPA axis). Nws tuaj yeem tswj hwm txoj haujlwm ntawm HPA axis thiab txo qhov tso tawm ntawm cov tshuaj hormones kev ntxhov siab xws li cortisol.
Kev nce qib ntawm cortisol tuaj yeem ua rau muaj kev ntxhov siab ntau ntxiv, thiab selanc txo cov tsos mob ntawm kev ntxhov siab los ntawm kev tawm tsam cov lus teb ntau dhau ntawm HPA axis thiab txo qis kev tso tawm cortisol.
Cov ntaub ntawv pov thawj los ntawm kev sim tsiaj thiab kev tshawb fawb soj ntsuam:
Hauv kev sim tsiaj, tom qab siv selanc ntawm kev ntxhov siab tus qauv tsiaj, lawv tau pom qhov txo qis hauv kev ntxhov siab xws li kev coj tus cwj pwm hauv kev ntsuam xyuas tus cwj pwm, piv txwv li kev nce hauv lub sij hawm nkag mus rau hauv qhib caj npab hauv qhov kev sim siab hla kev tshawb nrhiav thiab kev ua si ntau dua hauv kev sim qhib kev sim.
Cov kev tshawb fawb soj ntsuam kuj tau pom tias selanc muaj kev kho mob tseem ceeb rau cov neeg mob uas muaj kev ntxhov siab. Ib qho kev sim tshuaj ntsuam xyuas cov neeg mob uas muaj kev ntxhov siab dav dav pom tau tias tom qab kev kho mob nrog selanc, cov neeg mob 'Self Rating Anxiet Scale (SAS) tau qhab nia qis dua thiab muaj cov tshuaj tiv thaiv tsawg dua.
Qhov cuam tshuam rau kev kawm thiab kev nco:
Nws tuaj yeem txhawb kev loj hlob, sib txawv, thiab synaptic plasticity ntawm neurons. Nws tuaj yeem ua rau muaj kev nthuav qhia ntawm lub hlwb- muab tau los ntawm neurotrophic factor (BDNF), qhov tseem ceeb neurotrophic yam uas ua lub luag haujlwm tseem ceeb hauv kev ciaj sia, kev loj hlob, thiab kev sib txawv ntawm cov neurons. Los ntawm kev nce qib BDNF, kev sib txuas thiab cov ntaub ntawv xa mus ntawm cov neurons tuaj yeem txhim kho, yog li txhim kho kev kawm thiab kev nco muaj peev xwm. Hauv kev sim tsiaj, kev siv cov nas ua haujlwm tau zoo txhim kho lawv txoj kev kawm thiab kev nco ua haujlwm hauv kev sim maze, ua rau lawv nrhiav zaub mov lossis khiav tawm ntawm txoj kev tshawb nrhiav sai dua.
Qhov cuam tshuam rau kev saib xyuas thiab kev ua haujlwm:
Nws tseem tuaj yeem txhim kho kev mloog zoo thiab kev ua haujlwm ua haujlwm. Nws tuaj yeem tswj hwm cov haujlwm ntawm lub paj hlwb ntawm lub paj hlwb, txhim kho kev sib koom ua ke ntawm cov neurons, thiab ua rau tib neeg tsom mus rau cov haujlwm.
Nyob rau tib lub sijhawm, nws tuaj yeem txhim kho lub luag haujlwm ntawm prefrontal cortex, uas yog lub hlwb tseem ceeb rau kev tswj hwm kev ua haujlwm, lub luag haujlwm rau kev paub txog kev ua haujlwm siab tshaj plaws piv txwv li kev txiav txim siab- ua, kev npaj, thiab kev tawm tsam. Txoj kev tshawb nrhiav pom tias tom qab siv, cov neeg koom nrog kev ua haujlwm tau zoo dua qub hauv kev saib xyuas thiab kev sim ua haujlwm ua haujlwm.
Muaj peev xwm mechanisms thiab kev kho mob daim ntawv thov kev cia siab:
Lub peev xwm txheej txheem uas selanc txhim kho kev txawj ntse kuj tseem tuaj yeem cuam tshuam txog kev tswj hwm neuroinflammation thiab oxidative kev nyuaj siab. Neuroinflammation thiab oxidative kev nyuaj siab tuaj yeem ua rau muaj kev puas tsuaj rau neuronal thiab kev paub tsis meej, thaum inhibiting kev tso tawm ntawm cov kab mob inflammatory tuaj yeem txo oxidative kev nyuaj siab thiab tiv thaiv cov neurons.
Hais txog kev siv tshuaj kho mob, nws yuav tsum tau siv los kho cov kab mob kev paub tsis meej xws li Alzheimer's kab mob thiab kev paub tsis meej me ntsis, tab sis tseem xav tau kev sim tshuaj ntxiv ntxiv los txheeb xyuas nws cov txiaj ntsig thiab kev nyab xeeb.
Qhov cuam tshuam rau lub cev tiv thaiv kab mob:
Nws tuaj yeem tswj cov kev ua haujlwm ntawm ntau lub cev tiv thaiv kab mob. Nws tuaj yeem txhim kho lub peev xwm phagocytic ntawm macrophages, uas yog thawj kab ntawm kev tiv thaiv hauv lub cev tiv thaiv kab mob thiab tuaj yeem cuam tshuam thiab tshem tawm cov kab mob thiab cov khoom txawv teb chaws. Nws tseem tuaj yeem txhawb kev loj hlob thiab kev sib txawv ntawm lymphocytes, txhim kho cov cellular thiab humoral tiv thaiv kev ua haujlwm ntawm lub cev. Piv txwv li, kev sim hauv vitro tuaj yeem ua rau muaj kev loj hlob ntawm T lymphocytes thiab B lymphocytes, thiab txhawb kev tsim cov tshuaj tiv thaiv.
Kev cai ntawm cytokines:
Cytokines ua lub luag haujlwm tseem ceeb hauv kev tiv thaiv kab mob. Nws tuaj yeem tswj hwm qhov zais cia ntawm cytokines, nce qhov tso tawm ntawm cov tshuaj tiv thaiv - inflammatory cytokines (piv txwv li interleukin -10), thiab txo qis kev tso tawm ntawm pro-inflammatory cytokines (piv txwv li qog necrosis factor alpha, interleukin-6).
Cov kev cai sib npaug ntawm cytokine secretion pab txo cov tshuaj tiv thaiv kab mob thiab tswj kev ruaj ntseg ntawm lub cev tiv thaiv kab mob.
Muaj peev xwm siv tau rau hauv cov kab mob tiv thaiv kab mob
Vim nws cov cuab yeej immunomodulatory, nws muaj peev xwm siv tau tus nqi hauv kev kho cov kab mob tiv thaiv kab mob. Piv txwv li, nyob rau hauv cov kab mob autoimmun, lub immue sytem qhov kev tawm tsam ntawm ib tus kheej cov ntaub so ntswg yuav txo tau los ntawm kev tswj cov kev ua ntawm cov tshuaj tiv thaiv kab mob thiab lub secretion ntawm cytokines; Hauv cov kab mob sib kis, nws tuaj yeem txhim kho kev tiv thaiv kab mob ntawm lub cev thiab txhim kho kev tiv thaiv kab mob.
Muaj pes tsawg tus neeg thiab ntau npaum li cas:
Haum rau cov neeg mob uas muaj ntau hom kev ntxhov siab, nrog rau kev ntxhov siab dav dav, kev ntxhov siab hauv kev sib raug zoo, kev ntxhov siab, thiab lwm yam. Cov tshuaj ntau npaum li cas rau cov neeg mob ntawm ntau pawg hnub nyoog thiab qhov hnyav ntawm tus mob. Cov koob tshuaj tuaj yeem maj mam hloov kho raws li tus neeg mob cov lus teb thiab kev ua siab ntev, tab sis feem ntau tsis tshaj 3mg ib hnub.
Txoj kev tswj hwm:
Selank hmoovfeem ntau yuav tsum tau yaj ua ntej siv. Hmoov tuaj yeem yaj hauv physiological saline los yog cov dej txhaj tshuaj los tsim ib qho kev daws teeb meem, thiab tom qab ntawd muab rau cov neeg mob los ntawm kev txhaj tshuaj subcutaneous, txhaj tshuaj intramuscular, lossis kev tswj qhov ntswg.
Kev tswj qhov ntswg yog ib txoj hauv kev yooj yim, vim tias cov tshuaj tuaj yeem nqus tau sai sai rau hauv cov hlab ntsha los ntawm qhov ntswg mucosa thiab siv cov tshuaj pharmacological.
Cov nyhuv kho thiab kev nyab xeeb
Cov kev tshawb fawb soj ntsuam tau pom tias nws muaj kev kho mob zoo rau cov neeg mob uas muaj kev ntxhov siab. Nws tuaj yeem txo cov neeg mob cov tsos mob ntxhov siab, txhim kho kev pw tsaug zog zoo, thiab txhim kho lawv lub neej zoo. Nyob rau tib lub sijhawm, nws muaj kev nyab xeeb siab thiab tsawg dua qhov tsis zoo. Cov tshuaj tiv thaiv tsis zoo muaj xws li mob thiab o ntawm qhov chaw txhaj tshuaj, uas feem ntau mob me me thiab tuaj yeem txo tau ntawm lawv tus kheej.
Daim ntawv thov hauv Alzheimer's disease:
Nyob rau theem pib ntawm Alzheimer's disease, nws tuaj yeem siv los ua cov tshuaj kho mob ntxiv. Nws tuaj yeem txhim kho cov neeg mob kev paub txog kev ua haujlwm xws li kev nco, kev xav, kev muaj peev xwm hais lus, thiab lwm yam, thiab ncua kev loj hlob ntawm tus kab mob. Txawm li cas los xij, tam sim no muaj kev tshawb fawb me me ntawm kev kho mob Alzheimer's kab mob hauv cov neeg laus, thiab xav tau kev sim tshuaj ntau ntxiv los txheeb xyuas nws lub sijhawm ntev - kev ua tau zoo thiab kev nyab xeeb.
Daim ntawv thov hauv kev puas hlwb me me:
Rau cov neeg mob uas muaj kev puas siab puas ntsws me me, nws tuaj yeem pab txhim kho kev paub txog kev ua haujlwm thiab tiv thaiv kev puas tsuaj ntxiv. Qee qhov kev tshawb fawb soj ntsuam ua ntej tau pom tias tom qab kev kho mob, cov neeg mob cov qhab nia kev txawj ntse txhim kho thiab lawv lub peev xwm ua neej nyob txhua hnub.
Kev siv rau hauv cov kab mob autoimmune:
Nws tuaj yeem siv los ua kev kho mob ntxiv rau hauv cov kab mob autoimmun xws li mob caj dab rheumatoid thiab kab mob lupus erythematosus. Nws tuaj yeem tswj cov haujlwm ntawm lub cev tiv thaiv kab mob, txo cov tshuaj tiv thaiv kab mob, thiab txo cov tsos mob. Txawm li cas los xij, kev siv cov khoom lag luam hauv kev kho cov kab mob autoimmune tseem nyob rau theem kev tshawb fawb, thiab kev sim tshuaj ntxiv yog xav tau los txiav txim siab nws cov txiaj ntsig thiab kev kho kom zoo.
Kev siv cov kab mob sib kis:
Hauv cov kab mob sib kis, nws tuaj yeem txhim kho kev tiv thaiv kab mob ntawm lub cev thiab txhim kho kev tiv thaiv kab mob. Piv txwv li, hauv kev kho mob ntawm qee yam kab mob kis kab mob, cov tshuaj tiv thaiv kab mob tuaj yeem pab txhim kho kev kho mob.
Kev sib piv ntawm selanc thiab lwm yam khoom zoo sib xws
Cov yam ntxwv thiab kev ua haujlwm
Lwm cov tshuaj peptide, piv txwv li pro phagocytic peptides thiab thymopentins, kuj muaj qee yam kev tiv thaiv kab mob thiab kab mob lom. Tab sisselank hmoovmuaj qhov tshwj xeeb tiv thaiv kev ntxhov siab thiab kev paub txog kev txhim kho uas lwm cov tshuaj peptide tsis muaj. Lub caij no, selanc muaj qhov ruaj khov thiab bioavailability, uas yog qhov zoo dua rau kev siv tshuaj kho mob.
Clinical daim ntawv thov Scope
Daim ntawv thov kev kho mob ntawm lwm cov tshuaj peptide yog qhov nqaim, feem ntau yog tsom rau hauv kev tswj hwm kev tiv thaiv kab mob. Selanc tuaj yeem siv tsis tau tsuas yog siv rau kev kho mob ntawm cov kab mob tiv thaiv kab mob, tab sis kuj rau kev kho mob ntawm ntau yam kab mob xws li kev ntxhov siab thiab kev paub tsis meej, nrog rau ntau yam kev siv tshuaj kho mob.
Kev Npaj thiab Kev Tswj Xyuas Zoo
Txoj kev npaj
Cov txheej txheem tshuaj synthesis
Tam sim no, selanc feem ntau yog npaj los ntawm chemical synthesis method. Cov txheej txheem tshuaj synthesis suav nrog ob txoj hauv kev tseem ceeb: cov khoom sib xyaw-theem synthesis thiab kua-theem synthesis. Cov txheej txheem sib xyaw ua ke yog cov txheej txheem ntawm kev sib txuas cov amino acids ib qho los ntawm ib qho mus rau kev txhawb nqa khoom, ua raws li cov tshuaj tiv thaiv kab mob thiab ntxuav cov kauj ruam kom kawg tshem tawm lub hom phiaj peptide los ntawm kev txhawb nqa. Kev sib xyaw ua kua theem muaj xws li kev sib txuas cov tshuaj tiv thaiv ntawm cov amino acids hauv kev daws, thiab kev sib txuas ntawm lub hom phiaj peptide tau ua tiav los ntawm kev tswj cov tshuaj tiv thaiv kab mob thiab kev siv cov pab pawg tiv thaiv. Cov txheej txheem tshuaj synthesis muaj qhov zoo ntawm kev tswj cov tshuaj tiv thaiv thiab cov khoom siab purity, tab sis cov txheej txheem synthesis yog qhov nyuaj thiab tus nqi siab.
Biosynthesis
Biological synthesis yog siv cov microbial lossis cell kab lis kev cai los tsim selanc. Piv txwv li, cov noob encoding selanc tuaj yeem nkag mus rau hauv cov kab mob lossis cov kab mob poov xab los ntawm kev siv thev naus laus zis thev naus laus zis, tso cai rau cov hlwb los qhia thiab zais cov selanc. Txoj kev biosynthetic muaj qhov zoo ntawm tus nqi qis thiab kev tiv thaiv ib puag ncig, tab sis tseem muaj teeb meem piv txwv li kev qhia qis thiab kev ua kom huv ntawm cov khoom nyuaj, uas yuav tsum tau tshawb xyuas ntxiv thiab ua kom zoo dua qub.
Kev tswj kom zoo
Kev kuaj purity
Purity yog ib qho tseem ceeb ntawm kev ntsuas qhov zoo ntawm selanc Cov kev ntsuas purity Feem ntau muaj xws li siab -kev ua haujlwm ua kua chromatography (HPLC), huab hwm coj spectrometry, thiab lwm yam. HPLC tuaj yeem cais thiab txheeb xyuas cov ntsiab lus ntawm txhua qhov khoom hauv ib qho qauv raws li qhov sib txawv ntawm kev faib coefficients ntawm cov theem nyob ruaj khov thiab txawb. Mass spectrometry tuaj yeem txiav txim siab qhov hnyav molecular thiab cov ntaub ntawv ntawm cov khoom, ntxiv kev txheeb xyuas qhov purity thiab qauv ntawm selanc.
Kev txiav txim siab txog cov ntsiab lus
Kev txiav txim siab cov ntsiab lus hais txog kev txiav txim siab cov ntsiab lus ntawm selanc hauv selanc. Kev txheeb xyuas ntau txoj hauv kev piv txwv HPLC ua ke nrog cov txheej txheem sab nraud lossis sab hauv feem ntau yog siv los txiav txim. Los ntawm kev sib piv nrog cov qauv qauv, suav cov ntsiab lus ntawm selanc hauv cov qauv kom ntseeg tau tias nws ua tau raws li cov qauv kev cai.
Kev tsom xam impurity
Kev tsom xam impurity yog ib feem tseem ceeb ntawm kev tswj kom zoo. Ua tau impurities hauvSelank hmoovsuav nrog unreacted amino acids, los ntawm -cov khoom, degradation cov khoom, thiab lwm yam. Kev soj ntsuam zoo thiab ntau yam ntawm impurities yog ua los ntawm cov txheej txheem piv txwv li HPLC thiab huab hwm coj spectrometry los tswj cov ntsiab lus ntawm impurities nyob rau hauv ib qho kev nyab xeeb ntau yam, kom ntseeg tau qhov zoo thiab kev nyab xeeb ntawm selanc.
Qhov tsis yog classical binding hom ntawm Selank thiab GABA receptors
Selank hmoovyog cov tshuaj heptapeptide hluavtaws nrog cov kab ke Thr Lys Pro Arg Pro Gly Pro (TKPRPGP), uas txhim kho kev ruaj ntseg los ntawm kev ua raws li endogenous tetrapeptide Tuftsin (Thr Lys Pro Arg) thiab ntxiv ib qho proline glycine proline (PGP) tripeptide fragment. Raws li cov tshuaj tiv thaiv kev ntxhov siab, Selank qhov tshwj xeeb yog nyob rau hauv nws cov txheej txheem ntawm kev ua, uas tsis yog tsuas yog cuam tshuam nrog cov tshuaj neurotransmitter ib txwm muaj (xws li serotonin thiab dopamine), tab sis kuj cuam tshuam nrog gamma aminobutyric acid (GABA) receptors los ntawm tsis yog classical txhais tau tias. GABA yog lub ntsiab inhibitory neurotransmitter hauv nruab nrab paj hlwb, thiab nws cov receptors (GABA_A thiab GABA_B) yog lub hom phiaj tseem ceeb ntawm cov tshuaj tiv thaiv kev ntxhov siab xws li benzodiazepines thiab barbiturates. Txawm li cas los xij, txoj kev khi ntawm Selank rau GABA receptors yog qhov sib txawv ntawm cov ligands ib txwm muaj, pom tau tias tsis muaj kev sib raug zoo, tsis muaj kev sib tw, thiab ntau yam - cov txiaj ntsig sib koom ua ke.
Lub hauv paus txheej txheem thiab classical binding hom ntawm GABA receptors
Structure thiab Function ntawm GABA_A Receptor
GABA_A receptors belongs rau ligand gated ion channel superfamily, muaj tsib subunits (1-6, 1-3, 1-3, δ, ε, θ, π) tsim ib tug pentamer qauv. Classic khi qhov chaw muaj xws li:
Qhov zoo tshaj plaws allosteric regulatory site (BZD site): nyob ntawm alpha/gamma subunit interface, nws yog ib qho chaw khi rau benzodiazepines (xws li diazepam), uas ua rau sedative thiab tiv thaiv kev ntxhov siab los ntawm kev txhim kho GABA induced chloride ion influx.
GABA binding site: nyob rau hauv lub extracellular domain ntawm lub beta subunit, nws yog ib tug endogenous GABA binding site uas ncaj qha activates receptor raws.
Ethanol / steroid binding site: nyob ntawm alpha / beta subunit interface, kho cov kev tswj hwm ntawm ethanol thiab neuroactive steroids.
Structure thiab Function ntawm GABA_B Receptors
GABA_B receptor yog G protein ua ke receptor (GPCR) tsim los ntawm heterodimer ntawm GABA_B1 (binding subunit) thiab GABA_B2 (effector subunit). Classic khi qhov chaw muaj xws li:
GABA binding site: nyob rau hauv Venus flytrap domain ntawm GABA_B1, nws ncaj qha khi rau GABA thiab induces receptor conformational hloov.
Qhov zoo tshaj plaws allosteric regulatory site: nyob rau hauv lub transmembrane domain ntawm GABA_B2, nws yog ib tug binding site rau cov tebchaw xws li CGP7930, uas yuav txhim khu lub teeb liab transduction ntawm GABA_B receptors.
Kev khi cov yam ntxwv ntawm classical ligands
Tsoos GABA receptor modulators (xws li benzodiazepines, barbiturates, thiab baclofen) ncaj qha lossis ncaj qha tswj hwm kev ua haujlwm receptor los ntawm kev khi rau cov chaw tshwj xeeb uas muaj kev sib raug zoo thiab kev sib tw. Piv txwv li, diazepam txhim kho GABA_A receptor muaj nuj nqi los ntawm kev khi rau BZD site, thaum baclofen inhibits adenylate cyclase (AC) kev ua los ntawm activating GABA_B receptors.
|
|
|
Qhov tsis yog classical binding hom ntawm Selank thiab GABA receptors
Tsawg affinity thiab ntau- lub hom phiaj khi:Molecular docking thiab deg plasmon resonance (SPR) cov kev tshawb fawb tau pom tias Selank tau txo qis affinity rau GABA_A thiab GABA_B receptors piv rau classical ligands xws li diazepam lossis GABA nws tus kheej. Nws qhov dissociation tas li (Kd) feem ntau yog nyob rau hauv micromolar (μ M) ntau yam, thaum cov ligands ib txwm muaj ib tug nanomolar (nM) ntau. Qhov kev sib raug zoo qis no qhia tias Selank tuaj yeem siv nws cov txiaj ntsig los ntawm cov hauv qab no:
Ntau lub hom phiaj kev sib koom ua ke: Selank tuaj yeem khi ib txhij rau / subunit interface ntawm GABA_A receptor thiab GABA_B1 / GABA_B2 heterodimer interface ntawm GABA_B receptor, tsim "ntau- taw tes tiv tauj" kev tswj hwm network.
Dynamic binding: Tsawg affinity binding tso cai rau Selank sai khi thiab dissociate ntawm physiological concentrations, ua tiav dynamic kev cai ntawm receptor muaj nuj nqi es tsis txhob ua kom muaj zog / inhibition.
Tsis muaj kev sib tw tswj kev tswj hwm:Selank txoj cai ntawm GABA receptors nthuav tawm cov yam ntxwv tsis sib tw, txhais tau tias nws cov txiaj ntsig tsis hloov pauv nrog kev hloov pauv hauv GABA concentration. Cov qauv no yog qhov sib txawv ntawm cov kev sib tw classical xws li kev tswj hwm ntawm GABA_A receptors los ntawm clopidogrel.
Kev tswj hwm kev sib txawv: Selank tuaj yeem khi rau qhov chaw conformational ntawm beta thiab gamma subunits ntawm GABA_A receptors, los yog lub transmembrane domain ntawm GABA_B receptors (TM3-TM6), indirectly txhim kho affinity los yog teeb liab transduction efficiency ntawm GABA los ntawm inducing receptor conformation.
Receptor subunit selectivity: Selank nthuav tawm kev xaiv ntau dua ntawm 2/3 subunits ntawm GABA_A receptor (txuas nrog kev tiv thaiv kev ntxhov siab), es tsis yog qhov chaw BZD classical (sib qhia los ntawm 1/ 2/ 3/ 5 subunits), uas yuav piav qhia nws qhov tsis muaj cov kev mob tshwm sim hauv kev ntxhov siab.
Dynamic adaptability ntawm peptide conformation:Raws li ib tug saj zawg zog heptapeptide, Selank nthuav tawm heev dynamic conformation nyob rau hauv cov kev daws teeb meem, muab lub hauv paus rau nws tsis classical binding nrog GABA receptors.Qhov rigidity ntawm proline residues: Selank muaj peb proline (Pro) residues (Pro4, Pro6, Pro7), tsim ib lub zos ua hauj lwm rigid qauv ntawm lub cheeb tsam. receptor.Slexible kev twb kev txuas ntawm glycine: Gly5 ua hauj lwm raws li ib tug saj zawg zog kev twb kev txuas taw tes, cia Selank kho nws conformation hloov mus rau lub receptor nto topology thaum khi.
Molecular dynamics simulation: Lub simulated binding ntawm Selank thiab GABA_A receptor 2 subunit tau pom tias nws N-terminus (Thr1-}Lys2) tsim hydrogen bonds nrog lub voj extracellular (ECL1) ntawm lub receptor, thaum nws C-terminus (PGP TM phosphorbic 2) kev sib cuam tshuam. bipolar binding 'hom tso cai rau Selank zawv zawg rau ntawm qhov chaw receptor thiab dynamically kho qhov chaw sib khi kom ua kom zoo dua cov kev cai.
Synergistic nyhuv nrog endogenous regulatory molecules:Selank tuaj yeem tsim cov haujlwm ua haujlwm nrog GABA receptors los ntawm simulating cov qauv kev tswj hwm ntawm endogenous neuropeptides xws li neuropeptide Y thiab thyrotropin tso cov tshuaj hormones.
Co immunoprecipitation sim: Selank kev kho mob tuaj yeem txhim kho qhov kev sib koom ua ke ntawm GABA_A receptor thiab neuropeptide Y receptor Y1 subtype, tawm tswv yim tias ob qho tib si tuaj yeem tswj hwm neuronal excitability los ntawm kev tsim cov heterologous complexes.
Kev Sib Tham Sib Tham Sib Tham: Tom qab Selank qhib GABA_B receptors, nws tuaj yeem txhim kho kev tso tawm ntawm lub hlwb - tau txais txiaj ntsig neurotrophic (BDNF), uas nws tus kheej tuaj yeem tswj hwm GABAergic neuron txoj kev loj hlob los ntawm TrkB receptors, tsim cov lus qhia zoo.
Cov lus nug nquag
Nws xav li cas rau hauv Selank?
Selank feem ntau ua rau koj hnov zoo, tsis tshua muaj kev ntxhov siab, thiab tsom mus rau ntau dua, ua haujlwm zoo li tus neeg nyob ntsiag to tab sis tsis tsaug zog, los ntawm kev txo qis kev ntxhov siab, ntshai, thiab kev ua phem thaum txhim kho kev txawj ntse xws li kev nco thiab kev mloog. Cov neeg siv feem ntau qhia txog kev thaj yeeb nyab xeeb, kev zoo siab (tshuaj tiv thaiv kev ntxhov siab), kev ntxhov siab zoo dua, thiab kev xav kom pom tseeb, vim nws ua haujlwm los ntawm kev hloov pauv cov neurotransmitters xws li GABA, dopamine, thiab serotonin, thiab txhawb lub hlwb- tau txais txiaj ntsig neurotrophic (BDNF).
Selank puas ua rau koj tsaug zog?
+
-
Tsis yog - nws calms lub siab yam tsis ua rau koj tsaug zog, yog li nws zoo meej rau kev siv nruab hnub. Selank puas muaj kev nyab xeeb rau kev siv txhua hnub? Yog lawm. Nws yog qhov zoo - zam thiab haum rau kev siv sijhawm ntev - raws li kev taw qhia kev tshaj lij.
Selank puas ua rau koj siab?
+
-
Qhov tshwm sim?Kev xav zoo dua, kev txawj ntse dua, thiab txhim kho kev puas siab ntsws. Selank tsis yog - sedating, tsis yog -เสพ, thiab zoo- zam los ntawm cov tib neeg feem coob, ua rau nws zoo dua rau kev kho mob ntxhov siab.
Vim li cas hydroxyzine ua rau kuv zoo siab heev?
+
-
Nws zoo ib yam li koj xav li cas tom qab noj Benadryl lossis NyQuil. Tab sis yuav ua li cas nws ua haujlwm rau kev ntxhov siab tau ua nroghydroxyzine cov teebmeem ntawm serotonin - cov tshuaj uas ua lub luag haujlwm hauv lub siab. Tsis zoo li lwm cov tshuaj tiv thaiv kab mob, hydroxyzine tuaj yeem pab txhawb qib serotonin hauv lub hlwb los kho kev ntxhov siab.
Cim npe nrov: selank hmoov, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom