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1kits （10Ibikoresho）
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IpamorelinStructure Imiterere ya
Inkomoko: PubChem |
Urukurikirane: XHXFK Inzira ya molekulari: C 38H 49N 9O.5 Uburemere bwa molekuline: 711.9 g / mol Numero ya CAS: 170851-70-4 PubChem CID: 9831659 Synonyme: NNC-26-0161 ； UNII-Y9M3S784Z6 AC IPAMORELIN ACETATE |
Research Ubushakashatsi bwa Ipamorelin
Ni ubuhe bushakashatsi bwakozwe na Ipamorelin?
Gutinda gukuramo gastrici ni ibintu bisanzwe, kandi kuri ubu, hari uburyo bwiza bwo kuvura. Ubushakashatsi bwerekanye ko Ipamorelin, nka peptidomimetike ikora, ikora kuri reseptor ya ghrelin kandi ishobora kugira ingaruka zo kuvura gutinda kwa gastrici. Mu bushakashatsi bwakozwe ku cyitegererezo cy’imbeba ya gastroparesis, gastroparesis yatewe no kubaga inda no gukoresha amara, kandi byagaragaye ko Ipamorelin ishobora kwihutisha gusiba gastric [1].
Ileus nyuma yibikorwa ni ikibazo gikomeye mubikorwa byubuvuzi, bidafite ingamba zifatika zo kuyobora. Ghrelin reseptor stimulation igira ingaruka-itera imbaraga kubice byo hejuru no hepfo byinzira ya gastrointestinal. Nka ghrelin reseptor agonist, Ipamorelin ifite agaciro gashobora gukoreshwa mukuvura ileus nyuma yo kubagwa. Kurugero, mubushakashatsi bwakozwe, ubushakashatsi buteganijwe, buteganijwe, bugenzurwa nubushakashatsi bwakozwe ku barwayi barimo kubagwa amara nyuma yo kubagwa mu nda kugirango basuzume umutekano n’akamaro ka Ipamorelin [2].
Ipamorelin ni iy'imisemburo ikura irekura peptide (GHRPs), ikaba ari pentapeptide ya sintetike ishobora gutera imbaraga zo gusohora imisemburo ikura ikomoka kuri hypothalamus na glande ya pitoito. Imisemburo ikura igira uruhare runini mu mikurire y’umubiri, gusana, no guhindagurika, bityo uruhare rwa Ipamorelin mu kugenga imisemburo ikura na rwo rwashimishije abantu benshi [3].
Bitewe n'akamaro kayo mu kuvura gutinda kwa gastrica gutinda, ileus nyuma yo kubagwa, n'uruhare rwayo nka hormone yo gukura irekura peptide, Ipamorelin yakunze ubushakashatsi cyane.
Nubuhe buryo bwo gukora bwa Ipamorelin?
1. Gukangurira gusohora imisemburo ikura:
Ipamorelin ni iy'imisemburo ikura irekura peptide (GHRPs), ishobora gutera imbaraga zo gusohora imisemburo ikura muri hypothalamus na glande ya pitoito. Muri vitro no mubushakashatsi bwa vivo, Ipamorelin yerekanye imbaraga nyinshi ningirakamaro mukurekura imisemburo ikura. Kurugero, mubushakashatsi bwakozwe, imbaraga nimbaraga za Ipamorelin mukurekura imisemburo ikura mumasemburo yibanze ya pitoito yari imeze nka GHRP-6 [3] . Uburyo bwibikorwa ni ugukangurira gusohora imisemburo ikura mugukoresha reseptor zimeze nka GHRP. Binyuze mu isesengura rya farumasi, hemejwe ko nka GHRP-6, Ipamorelin itera kurekura imisemburo ikura binyuze muri reseptor zimeze nka GHRP.
2. Ingaruka ku nzira ya gastrointestinal
Kwihutisha ubusa gastric:
Muburyo bwimbeba, Ipamorelin irashobora kwihuta gusiba gastric. Kubaga mu nda biganisha ku gutinda kwa gastrici gutinda, ariko nyuma yubuyobozi bwa Ipamorelin (0.014 µmol / kg imitsi), gusiba byihuta cyane. Ipamorelin itera kwandura gastric kandi yihutisha gusohora gastrici binyuze muburyo bwahujwe no gukora reseptor ya ghrelin, irimo neuron ya cholinergic ishimishije (Greenwood-Van Meerveld B, 2012).
Kunoza ibimenyetso bya ileus nyuma yo kubagwa:
Muburyo bwimbeba ya ileus nyuma yibikorwa, Ipamorelin irashobora kunoza ibimenyetso. Nyuma yubuyobozi bwa Ipamorelin nyuma yubuvuzi, ikinini kimwe cya Ipamorelin (1mg / kg) cyangwa GHRP-6 (20μg / kg) gishobora kugabanya igihe cyo kwiyuhagira bwa mbere. Gusubiramo inshuro nyinshi Ipamorelin (0.1 cyangwa 1mg / kg) birashobora kongera cyane umusaruro mwinshi wa fecal, gufata ibiryo, no kongera ibiro [4].
3. Ingaruka ku gusohora kwa insuline
Ipamorelin irashobora gutera insuline mu bice bya pancreatic tissue ibice byimbeba zisanzwe na diyabete. Ubwiyongere bw'isohoka rya insuline buterwa na Ipamorelin burashobora guhagarikwa cyane na diltiazem, yohimbine, propranolol, cyangwa guhuza atropine, propranolol, na yohimbine. Imbeba za diyabete, atropine irashobora kugabanya cyane imisemburo ya insuline iterwa na Ipamorelin, ariko iyi ngaruka ntabwo igaragara mu mbeba zisanzwe. Ibi byerekana ko Ipamorelin itera insuline ikoresheje umuyoboro wa calcium n'inzira ya reseptor ya adrenergic [5].
4. Kugabanya ububabare
Muburyo bwubushakashatsi bwa hypersensitivite ya visceral na inflammatory allodynia, Ipamorelin, nka ghrelin reseptor agonist yagabanijwe, irashobora kugabanya cyane hyperensitivite ya colonike na allodynia. Uburyo bwibikorwa byabwo bwahujwe na reseptor ya ghrelin, kandi izo ngaruka zirwanya anticociceptive zirashobora guhagarikwa na ghrelin reseptor antagonist H0900 [6].
S uburyo ingaruka za ipamorelin ku gusohora kwa insuline ziva mu bice bya pancreatic tissue ibice byimbeba zisanzwe na diyabete.
Inkomoko: PubMed [5]
Ni ubuhe buryo bukoreshwa na Ipamorelin?
1. Guteza imbere kurekura imisemburo ikura
Ipamorelin irashobora gutuma habaho gusohora imisemburo ikura muri hypothalamus na glande ya pitoito. Imisemburo ikura igira uruhare runini mu mubiri w'umuntu, harimo guteza imbere intungamubiri za poroteyine, ikwirakwizwa ry'uturemangingo, no gusana ingirangingo. Kubwibyo, Ipamorelin irashobora gukoreshwa mukuvura kubura imisemburo ikura cyangwa izindi ndwara zijyanye no kubura imisemburo ikura [7].
2. Kunoza imikorere ya gastrointestinal
Kwihutisha ubusa gastric:
Muburyo bwimbeba, Ipamorelin yihutisha gusohora gastrica muburyo bwa ileus nyuma yo kubagwa hakoreshejwe uburyo bwahujwe no gukora imisemburo ikura irekura peptide reseptor, irimo na neuron ya cholinergique itera imbaraga [1] . Kubaga inda biganisha ku gutinda kwa gastrici gutinda, kandi ubuyobozi bwa Ipamorelin burashobora kugabanya cyane igipimo cyibiribwa bisigaye mu gifu, bityo bikagenda neza.
Guteza imbere gastrointestinal peristalsis:
Muburyo bwimbeba ya ileus nyuma yo kubagwa, Ipamorelin irashobora kunoza ibimenyetso byabarwayi. Kurugero, muburyo bwimbeba, Ipamorelin irashobora kugabanya igihe cyo kwandura bwa mbere nyuma yo kubagwa, kongera umusaruro wa fecal, gufata ibiryo, no kongera ibiro [4] . Gusubiramo inshuro nyinshi Ipamorelin birashobora kongera cyane umusaruro mwinshi wa fecal, gufata ibiryo, no kongera ibiro, byerekana ingaruka nziza zogukora kumikorere ya gastrointestinal.
3. Kugabanya ububabare
Kugabanya ububabare bwa visceral na somatike:
Ubushakashatsi bwerekana ko Ipamorelin, nka hormone yo gukura irekura peptide reseptor agonist, ifite imiti igabanya ubukana. Mubitegererezo byubushakashatsi bidafite epiteleial colonique, Ipamorelin irashobora kugabanya cyane hyperensitivite ya visceral visceral hypermensitivite na allodynia ya somatike [6].
Uburyo bwibikorwa byabwo bushobora guhuzwa na hormone yo gukura irekura peptide reseptor, ikagira uruhare mukugenzura hyperensitivite ya visceral na somatike, itanga uburyo bushya bwo kuvura ububabare bukabije bwimyanya ndangagitsina na somatike.
Ni ubuhe bushakashatsi bwakozwe na Ipamorelin mu kuvura kubura imisemburo ikura?
Gukura imisemburo ya hormone ni indwara iterwa no gusohora kudahagije imisemburo ikura iva mu mitsi ya pitoito y'imbere, ishobora kugira ingaruka ku mikurire no gukura kw'abana ndetse no guhindagurika k'umubiri w'abantu bakuru. Mu myaka yashize, Ipamorelin, nk'imisemburo ikura ya secretagogue, yakunze kwitabwaho cyane mu kuvura ibura ry'imisemburo ikura. Ibikurikira niterambere ryubushakashatsi bwa Ipamorelin mukuvura kubura imisemburo ikura.
1. Ingaruka zikangura Ipamorelin kumisemburo ikura
Ipamorelin irashobora gutuma imisemburo ikura. Ubushakashatsi bwerekana ko Ipamorelin ishobora gukorana hamwe na hormone yo gukura irekura imisemburo (GHRH) kugirango yongere imisemburo ikura [8] . Mu bushakashatsi bw’inyamaswa, nyuma yiminsi 21 yo kuvura karande hamwe na Ipamorelin mu mbeba z’abakobwa bakiri bato, ugereranije n’itsinda rishinzwe kugenzura, imisemburo yo gukura y’ibanze mu muco wa monolayeri y’ingirabuzimafatizo ya pitoito yariyongereye. Muri icyo gihe, Ipamorelin na GHRH birashobora gutuma habaho gusohora imisemburo ikura ituruka mu ngirabuzimafatizo zifite imiterere ya vitro. Icyakora, mu itsinda ryitegura rya GHRH, imisemburo yo gukura nyuma y’imisemburo yo gukangura ntiyigeze yongerwa, mu gihe mu itsinda ry’imyitozo ya Ipamorelin, nta kintu na kimwe cyigeze kibaho, byerekana ko Ipamorelin itatuma habaho kwanduza imisemburo ikura ku mbeba z’abakobwa bakiri bato [8].
2. Ingaruka za Ipamorelin mukongera ibiro
Imiyoborere idakira ya Ipamorelin irashobora kongera uburemere bwimbeba zimbeba zabakobwa. Igenzura rya buri munsi ryerekana ko ijanisha ryiyongera ryibiro mu itsinda ryitegura Ipamorelin hamwe nitsinda rya GHRH ryitondewe rirenze iryo mu itsinda rishinzwe kugenzura [8] . Ibi bifitanye isano nuko Ipamorelin itera ururenda rwa hormone yo gukura, ari nako rutera intungamubiri za poroteyine no gukura kwa selile.
3. Ingaruka ya Ipamorelin kumiterere yamagufwa
Mu buryo bw'imbeba ikuze, byagaragaye ko imisemburo ikura ya secretagogue Ipamorelin ishobora kurwanya ingaruka za catabolike ya glucocorticoide (GC) ku mitsi ya magufa n'amagufwa. Ugereranije n'itsinda ryatewe na GC ryonyine, mu nyamaswa zatewe na GC na Ipamorelin, impagarara nyinshi za tetanike z'imitsi y'inyana ziyongereye ku buryo bugaragara, kandi igipimo cy'amagufwa ya periosteal cyiyongereyeho kane [8, 9] . Ibi byerekana ko Ipamorelin igira ingaruka nziza mukubungabunga imbaraga zimitsi no guteza imbere amagufwa, kandi irashobora gufasha kwirinda ingorane nka osteoporose kubarwayi bafite imisemburo ikura.
4. Ingaruka za Ipamorelin kumikorere ya gastrointestinal
Ipamorelin nk'imisemburo ikura irekura imisemburo ya agonist hamwe na hormone ikura ya peptide reseptor agonist, Ipamorelin yerekanye uburyo bwo kuvura muburyo bwimbeba yerekana ubumuga bwo mu nda nyuma yo kubagwa. Ubuyobozi bumwe bwa Ipamorelin cyangwa imisemburo ikura ya peptide (GHRP) -6 yagabanije igihe cyo gutangira amara ya mbere nyuma yo kubagwa, ariko ntibyagize ingaruka ku musemburo wa fecal, gufata ibiryo, cyangwa kongera ibiro. Ipamorelin yongera umusaruro mwinshi wa fecal, gufata ibiryo, no kongera ibiro. Ibi byerekana ko Ipamorelin ishobora kugira uruhare runini mugutezimbere imikorere ya gastrointestinal kandi ishobora gufasha kunoza imikorere yigifu no kwinjiza abarwayi bafite imisemburo ikura. [4].
Muri make, nk'imisemburo ikura ikura imisemburo ikura, Ipamorelin itera imbaraga cyane kurekura imisemburo ikura ikora imisemburo ikura ya peptide reseptor (reseptor ya GHS), itagize ingaruka zikomeye kurwego rwa hormone adrenocorticotropique (ACTH) na cortisol. Mubikorwa byayo harimo guteza imbere imisemburo ikura, kugabanya umuvuduko wa gastrointestinal, no kugabanya ububabare. Guhitamo kwinshi hamwe nibiranga intego nyinshi bitanga ubushobozi bwo kuvura, bigatuma bikoreshwa mugihe nko kubura imisemburo ikura, guhagarika amara nyuma yo kubagwa, no gucunga ububabare.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Raun K ni umushakashatsi ufatanije na kaminuza ya tekinike ya Danemarke (DTU) na Fondasiyo ya Novo Nordisk. Inyungu zubushakashatsi bwe zikubiyemo amasomo menshi, harimo Endocrinology & Metabolism, Orthopedics, Imirire & Dietetics, Science Veterinary Science, naEngineering. Ibikorwa bye bikunze kwibanda ku iterambere ryibisubizo birambye kandi bishya, cyane cyane mubijyanye nubumenyi bwibinyabuzima nubukungu bushingiye kuri bio.
Raun K yagize uruhare mu mishinga ijyanye n’ikigo cya Novo Nordisk Foundation gishinzwe kubungabunga urusobe rw’ibinyabuzima muri DTU, igamije guteza imbere igishushanyo mbonera cy’inganda, ubwubatsi bwa metabolojiya, hamwe n’ibinyabuzima byifashishwa mu binyabuzima birambye. Byongeye kandi, yagize uruhare mu bushakashatsi bugamije kugabanya gushingira ku bikoresho bishingiye ku myanda no guteza imbere inzibacyuho binyuze mu bisubizo by’ibinyabuzima.
Ibikorwa bye binareba no mubikorwa byubwubatsi, nko guteza imbere catalizator na bioprocesses kugirango inganda n’ibidukikije bibungabungwa. Uburyo butandukanye bwa Raun K buhuza ubushakashatsi bwa siyansi n’uburyo bukoreshwa, butanga umusanzu ukomeye haba mu masomo n’inganda. Raun K yanditse kurutonde rwerekana [3].
