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1 khoom (10Vials)
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▎ Ipamorelin Structure
Source: PubChem |
Sequence: XHXFK Molecular Formula: C 38H 49N 9O5 Molecular Luj: 711.9 g / mol CAS Nr .: 170851-70-4 PubChem CID: 9831659 Synonyms: NNC-26-0161; UNII-Y9M3S784Z6; IPAMORELIN ACETATE |
▎ Ipamorelin Kev Tshawb Fawb
Kev tshawb fawb keeb kwm ntawm Ipamorelin yog dab tsi?
Kev ua paug plab qeeb yog ib yam mob uas tshwm sim, thiab tam sim no, muaj ob peb txoj kev kho mob zoo. Kev tshawb fawb tau pom tias Ipamorelin, raws li ib tug hluavtaws peptidomimetic, ua rau ghrelin receptor thiab tej zaum yuav muaj ib tug kho nyhuv ntawm qeeb plab hnyuv. Hauv kev tshawb fawb ntawm tus nas qauv ntawm gastroparesis, gastroparesis raug ntxias los ntawm kev phais plab thiab plab hnyuv, thiab nws tau pom tias Ipamorelin tuaj yeem ua rau lub plab zom mov [1].
Postoperative ileus yog ib qho kev sib tw tseem ceeb hauv kev kho mob, tsis muaj cov tswv yim tswj xyuas zoo. Ghrelin receptor stimulation muaj kev txhawb nqa kev txhawb nqa ntawm ob qho tib si sab sauv thiab sab hauv ntawm txoj hnyuv. Raws li ghrelin receptor agonist, Ipamorelin muaj peev xwm thov tus nqi hauv kev kho mob tom qab phais ileus. Piv txwv li, nyob rau hauv ib txoj kev tshawb no, ib tug yav tom ntej, randomized, tswj pov thawj-ntawm-lub tswv yim txoj kev tshawb no tau ua nyob rau hauv cov neeg mob nyob rau hauv lub plab hnyuv resection tom qab phais plab los soj ntsuam kev nyab xeeb thiab kev ua tau zoo ntawm Ipamorelin [2].
Ipamorelin belongs rau txoj kev loj hlob hormone tso tawm peptides (GHRPs), uas yog ib tug hluavtaws pentapeptide muaj peev xwm txhawb kev tso tawm ntawm kev loj hlob hormone los ntawm lub hypothalamus thiab pituitary caj pas. Kev loj hlob hormone plays lub luag haujlwm tseem ceeb hauv lub cev kev loj hlob, kho, thiab cov metabolism, yog li lub luag haujlwm ntawm Ipamorelin hauv kev tswj hwm kev loj hlob hormone kuj tau txais kev saib xyuas thoob plaws [3].
Vim nws qhov muaj peev xwm muaj txiaj ntsig hauv kev kho mob qeeb hauv plab hnyuv, postoperative ileus, thiab nws lub luag haujlwm raws li kev loj hlob hormone tso tawm peptide, Ipamorelin tau nyiam kev tshawb fawb ntau.
Yuav ua li cas yog lub mechanism ntawm kev txiav txim ntawm Ipamorelin?
1. Stimulating tso tawm ntawm kev loj hlob hormone:
Ipamorelin belongs rau kev loj hlob hormone tso tawm peptides (GHRPs), uas tuaj yeem txhawb kev tso tawm cov tshuaj hormones loj hlob los ntawm hypothalamus thiab qog pituitary. Hauv vitro thiab hauv vivo kev sim, Ipamorelin tau pom muaj zog thiab ua tau zoo hauv kev tso tawm cov tshuaj hormones loj hlob. Piv txwv li, nyob rau hauv ib txoj kev tshawb no, lub hwj chim thiab kev ua tau zoo ntawm Ipamorelin nyob rau hauv tso tawm kev loj hlob hormone los ntawm thawj nas pituitary hlwb zoo ib yam li cov GHRP-6 [3] . Nws cov txheej txheem ntawm kev ua haujlwm yog los txhawb kev tso tawm ntawm kev loj hlob hormone los ntawm kev ua kom GHRP zoo li receptors. Los ntawm kev tshuaj xyuas tshuaj, nws tau raug lees paub tias zoo li GHRP-6, Ipamorelin txhawb kev tso tawm ntawm kev loj hlob hormone los ntawm GHRP-zoo li receptors.
2. Kev cuam tshuam rau lub plab zom mov
Accelerating plab hnyuv plab:
Hauv cov qauv nas, Ipamorelin tuaj yeem ua kom lub plab zom mov. Kev phais plab ua rau lub plab zom mov qeeb, tab sis tom qab kev tswj hwm ntawm Ipamorelin (0.014 µmol / kg intravenously), lub plab khoob tau nrawm heev. Ipamorelin stimulates gastric contractility thiab ua kom lub plab khoob los ntawm kev sib kho los ntawm kev ua kom cov ghrelin receptor, koom nrog cholinergic excitatory neurons (Greenwood-Van Meerveld B, 2012).
Txhim kho cov tsos mob ntawm postoperative ileus:
Hauv cov qauv nas ntawm kev ua haujlwm tom qab ileus, Ipamorelin tuaj yeem txhim kho cov tsos mob. Tom qab kev tswj hwm ntawm Ipamorelin tom qab noj mov, ib koob tshuaj Ipamorelin (1mg / kg) lossis GHRP-6 (20μg / kg) tuaj yeem txo lub sijhawm rau thawj zaug defecation. Rov ua dua kev tswj hwm ntawm Ipamorelin (0.1 lossis 1mg / kg) tuaj yeem ua rau muaj kev tso zis ntau ntxiv, noj zaub mov, thiab qhov hnyav nce [4].
3. Kev cuam tshuam rau kev tso tawm insulin
Ipamorelin tuaj yeem ua rau cov tshuaj insulin tso tawm hauv cov ntaub so ntswg ntawm lub txiav ntawm cov nas ib txwm muaj thiab mob ntshav qab zib. Kev nce hauv insulin secretion tshwm sim los ntawm Ipamorelin tuaj yeem cuam tshuam los ntawm diltiazem, yohimbine, propranolol, lossis kev sib xyaw ntawm atropine, propranolol, thiab yohimbine. Hauv cov nas mob ntshav qab zib, atropine tuaj yeem txo qis cov tshuaj insulin los ntawm Ipamorelin, tab sis qhov txiaj ntsig no tsis tau pom hauv cov nas ib txwm muaj. Qhov no qhia tau hais tias Ipamorelin txhawb nqa insulin tso tawm los ntawm calcium channel thiab adrenergic receptor txoj kev [5].
4. Txo qhov mob
Hauv kev sim ua qauv ntawm cov tsis-inflammatory visceral hypersensitivity thiab somatic mechanical allodynia, Ipamorelin, raws li ib qho peripheral txwv ghrelin receptor agonist, tuaj yeem txo qis colonic hypersensitivity thiab somatic allodynia. Nws cov txheej txheem ntawm kev txiav txim yog kho los ntawm ghrelin receptor, thiab cov nyhuv antinociceptive tuaj yeem thaiv los ntawm ghrelin receptor antagonist H0900 [6].
S yuav ua li cas cov nyhuv ntawm ipamorelin ntawm insulin tso tawm los ntawm cov kab mob pancreatic tawg ntawm cov nas ib txwm muaj thiab mob ntshav qab zib.
Source: PubMed [5]
Dab tsi yog daim ntawv thov ntawm Ipamorelin?
1. Txhawb kev tso tawm ntawm kev loj hlob hormone
Ipamorelin tuaj yeem txhawb kev tso tawm ntawm kev loj hlob hormone los ntawm hypothalamus thiab pituitary caj pas. Kev loj hlob hormone plays lub luag haujlwm tseem ceeb hauv tib neeg lub cev, suav nrog kev txhawb nqa cov protein synthesis, cell proliferation, thiab kho cov ntaub so ntswg. Yog li, Ipamorelin tuaj yeem siv los kho kev loj hlob hormone tsis txaus lossis lwm yam kab mob ntsig txog kev loj hlob hormone tsis txaus [7].
2. Txhim kho txoj hnyuv ua haujlwm
Accelerating plab hnyuv plab:
Hauv cov qauv nas, Ipamorelin accelerates plab hnyuv hauv cov qauv ntawm postoperative ileus los ntawm ib qho kev sib kho los ntawm kev ua kom lub cev loj hlob tso tawm peptide receptor, koom nrog cholinergic excitatory neurons [1] . Kev phais plab ua rau lub plab zom mov qeeb, thiab kev tswj hwm ntawm Ipamorelin tuaj yeem txo qhov feem ntawm cov zaub mov seem hauv plab, yog li txhim kho plab hnyuv.
Txhawb nqa plab hnyuv peristalsis:
Hauv cov qauv nas ntawm postoperative ileus, Ipamorelin tuaj yeem txhim kho cov tsos mob ntawm cov neeg mob. Piv txwv li, nyob rau hauv tus qauv nas, Ipamorelin tuaj yeem txo lub sij hawm mus rau thawj qhov quav tom qab phais, ua kom cov zis tso zis ntau ntxiv, noj zaub mov, thiab qhov hnyav nce [4] . Rov ua dua kev tswj hwm ntawm Ipamorelin tuaj yeem ua rau muaj txiaj ntsig ntau ntxiv, kev noj zaub mov kom tsawg, thiab qhov hnyav nce, qhia tias nws cov txiaj ntsig zoo rau kev ua haujlwm ntawm plab hnyuv.
3. Kho qhov mob
Relieving visceral thiab somatic mob:
Kev tshawb fawb qhia tau hais tias Ipamorelin, raws li ib tug loj hlob hormone tso peptide receptor agonist, muaj antinociceptive zog. Hauv kev sim ua qauv yam tsis muaj colonic epithelial o, Ipamorelin tuaj yeem txo qis qhov tsis zoo ntawm cov visceral hypersensitivity thiab somatic mechanical allodynia [6].
Nws cov txheej txheem ntawm kev ua haujlwm tuaj yeem kho los ntawm kev loj hlob hormone tso tawm peptide receptor, koom nrog kev tswj hwm ntawm visceral thiab somatic hypersensitivity, muab txoj hauv kev tshiab rau kev kho mob visceral thiab somatic mob.
Dab tsi yog qhov kev tshawb fawb ntawm Ipamorelin nyob rau hauv kev kho mob ntawm kev loj hlob hormone deficiency?
Kev loj hlob hormone deficiency yog ib yam kab mob uas tshwm sim los ntawm tsis txaus tso tawm ntawm kev loj hlob hormone los ntawm anterior pituitary caj pas, uas yuav cuam tshuam rau kev loj hlob thiab kev loj hlob ntawm cov me nyuam thiab lub cev metabolism ntawm cov neeg laus. Nyob rau hauv xyoo tsis ntev los no, Ipamorelin, raws li ib tug loj hlob hormone secretagogue, tau attracted ntau mloog nyob rau hauv kev kho mob ntawm kev loj hlob hormone deficiency. Cov hauv qab no yog cov kev tshawb fawb txog kev nce qib ntawm Ipamorelin hauv kev kho mob ntawm kev loj hlob hormone deficiency.
1. Cov nyhuv stimulating ntawm Ipamorelin ntawm kev loj hlob hormone secretion
Ipamorelin tuaj yeem txhawb kev tso tawm ntawm kev loj hlob hormone. Kev tshawb fawb qhia tau hais tias Ipamorelin tuaj yeem ua ke nrog kev loj hlob hormone tso tawm hormone (GHRH) los txhim kho qhov tso tawm ntawm kev loj hlob hormone [8] . Hauv kev sim tsiaj, tom qab 21 hnub ntawm kev kho mob ntev nrog Ipamorelin hauv cov poj niam hluas nas, piv nrog cov pab pawg tswj hwm, cov tshuaj basal loj hlob tso tawm hauv monolayer kab lis kev cai ntawm pituitary hlwb nce. Tib lub sijhawm, Ipamorelin thiab GHRH tuaj yeem txhawb kev tso tawm cov tshuaj hormones loj hlob los ntawm cov kab mob pituitary hauv vitro. Txawm li cas los xij, hauv pawg GHRH pretreatment, qhov kev loj hlob ntawm cov tshuaj hormones tom ntej rau kev txhawb nqa tsis tau txhim kho, thaum nyob hauv Ipamorelin pretreatment pawg, tsis muaj qhov tshwm sim desensitization, qhia tias Ipamorelin tsis ua rau desensitization ntawm cov tshuaj hormones loj hlob hauv cov poj niam nas [8].
2. Cov nyhuv ntawm Ipamorelin rau qhov hnyav nce
Kev tswj hwm ntev ntawm Ipamorelin tuaj yeem ua kom qhov hnyav ntawm cov poj niam hluas nas. Kev saib xyuas txhua hnub qhia tau hais tias feem pua ntawm qhov hnyav nce hauv Ipamorelin pretreatment pab pawg thiab GHRH pretreatment pawg yog siab dua li hauv pawg tswj hwm [8] . Qhov no muaj feem xyuam rau qhov tseeb tias Ipamorelin stimulates lub secretion ntawm kev loj hlob hormone, uas nyob rau hauv lem txhawb protein synthesis thiab cell loj hlob.
3. Cov nyhuv ntawm Ipamorelin rau kev tsim cov pob txha
Hauv cov qauv nas laus, nws tau pom tias qhov kev loj hlob hormone secretagogue Ipamorelin tuaj yeem tiv thaiv cov teebmeem catabolic ntawm glucocorticoids (GC) ntawm cov leeg pob txha thiab pob txha. Piv nrog rau cov pab pawg txhaj nrog GC ib leeg, nyob rau hauv cov tsiaj txhaj tshuaj GC thiab Ipamorelin, qhov siab tshaj plaws tetanic nro ntawm cov leeg nqaij nyuj nce ntxiv, thiab cov pob txha periosteal tsim tau nce plaub npaug [8, 9] . Qhov no qhia tau hais tias Ipamorelin muaj txiaj ntsig zoo rau kev tswj cov leeg nqaij thiab txhawb kev tsim cov pob txha, thiab tuaj yeem pab tiv thaiv cov teeb meem xws li pob txha pob txha hauv cov neeg mob uas tsis muaj kev loj hlob hormone.
4. Cov nyhuv ntawm Ipamorelin rau kev ua haujlwm ntawm plab hnyuv
Raws li kev xaiv kev loj hlob hormone-tso cov tshuaj hormone agonist thiab kev loj hlob hormone-tso peptide receptor agonist, Ipamorelin tau qhia txog kev kho mob zoo hauv tus nas qauv ntawm kev mob plab hnyuv tuag tes tuag taw. Ib qho kev tswj hwm ntawm Ipamorelin lossis kev loj hlob hormone-tso peptide (GHRP)-6 txo lub sijhawm rau thawj zaug kev ua haujlwm ntawm lub plab zom mov, tab sis tsis muaj kev cuam tshuam rau kev tso zis ntau ntxiv, noj zaub mov, lossis qhov hnyav nce. Ipamorelin nce fecal tso zis ntau, noj zaub mov, thiab hnyav nce. Qhov no qhia tau tias Ipamorelin tuaj yeem muaj lub luag haujlwm hauv kev txhim kho plab hnyuv thiab tuaj yeem pab txhim kho plab zom mov thiab nqus dej hauv cov neeg mob uas tsis muaj kev loj hlob hormone. [4].
Hauv cov ntsiab lus, raws li kev xaiv kev loj hlob hormone secretion txhawb nqa, Ipamorelin ua tau zoo txhawb kev tso tawm ntawm kev loj hlob hormone los ntawm kev ua kom muaj kev loj hlob hormone-tso peptide receptor (GHS receptor), tsis muaj kev cuam tshuam rau qib ntawm adrenocorticotropic hormone (ACTH) thiab cortisol. Nws cov haujlwm muaj xws li txhawb kev loj hlob hormone secretion, tswj lub plab hnyuv motility, thiab alleviating mob. Nws cov kev xaiv siab thiab cov yam ntxwv ntau lub hom phiaj pom zoo rau kev siv tshuaj kho mob muaj peev xwm, ua rau nws tsim nyog siv rau hauv cov xwm txheej xws li kev loj hlob hormone deficiency, postoperative plab hnyuv obstruction, thiab kev tswj mob.
Hais Txog Tus Sau
Cov ntaub ntawv hais saum toj no yog txhua yam tshawb fawb, kho thiab sau los ntawm Cocer Peptides.
Scientific Journal Author
Raun K yog tus kws tshawb fawb koom nrog Technical University of Denmark (DTU) thiab Novo Nordisk Foundation. Nws txoj kev tshawb fawb nyiam nthuav dav ntau yam kev qhuab qhia, suav nrog Endocrinology & Metabolism, Orthopedics, Nutrition & Dietetics, Veterinary Sciences, thiab Engineering. Nws txoj haujlwm feem ntau tsom mus rau kev txhim kho cov kev daws teeb meem zoo thiab tsim kho tshiab, tshwj xeeb hauv cov ntsiab lus ntawm biotechnology thiab bio-based kev lag luam.
Raun K tau pab txhawb rau cov haujlwm uas cuam tshuam nrog Novo Nordisk Foundation Center rau Biosustainability ntawm DTU, uas tau mob siab rau kev tsim kho cell Hoobkas tsim, metabolic engineering, thiab hluavtaws biology rau sustainable bioproduction. Tsis tas li ntawd, nws tau koom nrog hauv kev tshawb fawb pib los txo qis kev cia siab ntawm cov ntaub ntawv fossil thiab txhawb kev hloov pauv ntsuab los ntawm kev daws teeb meem bioproduction.
Nws txoj haujlwm tseem cuam tshuam txog kev siv engineering, xws li kev tsim cov catalysts thiab bioprocesses rau kev lag luam thiab ib puag ncig kev ruaj ntseg. Raun K txoj kev sib txuas lus txuas txuas txuas rau kev tshawb fawb thiab kev siv tswv yim, ua rau muaj txiaj ntsig zoo rau kev kawm thiab kev lag luam. Raun K tau teev nyob rau hauv qhov kev siv ntawm cov ntaub ntawv pov thawj [3].
