Ziconotide pobertate, adagulitsa ngati Prialt, ndi Amino Acid, peptidel toptide topdide, omwe amachititsa chidwi cha South Pacific Marie Cones Mamaso. Ndi woyamba wa gulu latsopano la neurotherapeutic, lolemba calcium ya a calcium (NCBB). Imakhala ndi ma carcium to n-mtundu wa secimeloniture calcium mu ma carnels ndi axon, poyankha zowonjezera zowonjezera zomwe sizingakule. Amawonetsedwa kwa odwala omwe ali ndi ululu waukulu yemwe amafunikira chithandizo chovuta komanso osalolera kapena osavomerezeka kapena bwino kwa njira zina analgesics kapena interthal morphin. "Inturaccal Ziconotide Plyaceate ndiwothandiza pakuchizira matenda a postherpecgia, kupweteka kokhudzana ndi nentombo, zopweteka za neuropathic, zopweteka, komanso zowawa."
Ziconotide pocetate ndi zopangidwa ω-Mⅶ conotoxin poyambirira adanenedwa ngati polypeptide ya alloucinogenic conotogenic. Amino Acid amakhala ndi acid 25 acids: Cys-Gly-Gys-a Ala-Cys-arr-Cys-ar-ar-ar-ar-ar-ar-ar-ar. Ntchito yamankhwala ya polypeptide iyi imadalira zomangira zolimba, ndipo kulumikizanaku ndi kofunikira kwa mabwalo. Kapangidwe ka 3 koloko ya Zictotide palyace kunapezeka ndi NMR. Boti la Suwalphide C1-C16, C80 ndi C20 ndi C15-C25 pindani polytetide mu ω-medction, kuwonetsa zikhalidwe za ω-banja. Kuphatikiza apo, khola la 3-strand limapezeka pa kapangidwe kake, lomwe limawonjezera kukhazikika kwake. Pamwamba pa poicyotide pocetate imawonetsa kuchuluka kwa hydrophilicity chifukwa cholumikizira ndi amino acid polarity.
Kapangidwe ka hiconotide pocemate kumawonetsa kuthekera kwake monga mankhwala: Choyamba, kutalika kwa amino acid motsatizana ndikupanga njira yogwiritsidwira ntchito yopanga kapangidwe kake ndi pulogalamu yamankhwala; Kachiwiri, hydrophilicity ya molekyulu imapangitsa kuti ikhale yosavuta kupanga mitundu ya mankhwala osokoneza bongo; Chachitatu, kukhazikika kwa piconotide poketate kungakhudzidwe ndi othandizira kapena ogwiritsa ntchito ogwiritsa ntchito ngati okosijeni chifukwa cha chomangira chovomerezeka ndi methionine pa udindo 12; Pomaliza, kukula kwake ndi hydrophilicity kumachepetsa kuthekera kwake kulowera minofu, kutanthauza kuti ziconotide pocepate amatha kuperekedwa mwachindunji kudera la ma cellular omwe akufuna kuti azigwiritsa ntchito bwino. Zochita za pharmacological
Intranzical Ziconotide poceaceate ndi yothandiza m'mitundu ina yopweteka, monga kupweteka kwamisala komanso kupweteka kwa neuropathic. Kuphatikiza apo, zotsatirazi zimalozanso momveka bwino kuti ziconotide pocetate zimakwaniritsa zotsatira zake za analgesic pochita chandamale cha N-Vscc.
Makina azachipatala a mankhwalawa sakudziwika. Kafukufuku wa nyama wawonetsa kuti amathamangitsidwa ndikuletsa njira ya calcium mu nersices ager inffent mitsempha yopanda masitima kuti athe kuganiza kuti akuvulala.
Kapangidwe ka zunitide poceace kuli zomangira zitatu zonyansa zitatu, ndikupanga mawonekedwe opindika komanso okhwima komanso okhala ndi malupu anayi a asymmetric. Izi zimapangitsa kuti mamake a NCCS ndi kusanza kwambiri komanso kusankhidwa, posinthana ndi kuchuluka kwa calcium ma ions ndikulepheretsa kumasulidwa kwa neurotral. Kafukufuku wa nyama wawonetsa kuti Ziconotide poceatete amatha kuchepetsa kupweteka mu mtundu woyesera mu mtundu wosinthika komanso modekha. Kuphatikiza apo, zoiconotide pocetate zimatha kukhala ndi zotsatira za zolaula. Akagwiritsidwa ntchito mwachindunji pamalopo ovulala a mitsempha, ziconotide pocertate amachepetsa kupweteka kwa marrralgesia ndipo amayambitsa kupweteka kwamakina, koma sikunakhudze mitsempha yabwinobwino. Ziconotide poketate sizinachititse kulekerera kwa analgesic chifukwa choperekedwa makoswe ndi jakisoni. Mosiyana ndi jakisoni, jekeseni ya zuctotical ya ziconotide poceatete sanakhazikitse matenda opumira m'makoswe pomwe mankhwala a antinocheket adagwiritsidwa ntchito. "Pambuyo inturathal makonzedwe a zicnotide poceacetate (1, 5, 7.5, kapena 10μg pa ola limodzi) mu odwala 24 Mu kafukufuku wa vitro adawonetsa kuti ziconotide poceheat pang'ono adatseka kutulutsidwa kwa NoPnsephone Popanda Kumasulidwa Kumasulidwa kwa Gaba ndi Glutamate, ndipo sanabisire Nicotinic Acetylcholine Acetylcholine
Post Nthawi: 2025-07-16