GHRP-2 ntsiav tshuajyog ib qho khoom tsim tawm hexapeptide hormone uas txhawb nqa lub pulsatile secretion ntawm endogenous GH los ntawm activating GHS -R nyob rau hauv lub hypothalamic pituitary axis, ua raws li qhov kev txiav txim ntawm ntuj ghrelin. Txawm hais tias nws daim ntawv qub yog khov - cov hmoov qhuav qhuav, uas yuav tsum tau txhaj tshuaj tom qab kev kho dua tshiab, nyob rau xyoo tas los no muaj cov khoom lag luam uas tau thov kom muaj gonadorel hauv cov ntsiav tshuaj.
Pralmorelin COA
GHRP-2 ntsiav tshuajyog ib qho kev sib xyaw ua ke hexapeptide, thiab nws txoj hauv kev tseem ceeb ntawm kev ua haujlwm yog nyob ib puag ncig tshwj xeeb khi rau ghrelin receptor (GHS-R, feem ntau suav nrog GHS-R1a thiab GHS-R1b, qhov twg GHS-R1a plays lub luag haujlwm tseem ceeb hauv kev tswj kev loj hlob hormone secretion). Tom qab nkag mus rau tib neeg lub cev, nws tuaj yeem khi ncaj nraim rau GHS-R1a receptor nyob rau saum npoo ntawm lub cev pituitary, thiab cov txheej txheem kev khi no zoo li tus yuam sij qhib lub kaw lus tshwj xeeb, ua rau muaj kev cuam tshuam ntawm intracellular signaling cascades.
Tshwj xeeb, receptor activation tom qab khi txhawb kev qhib cov calcium hauv lub cev, ua rau calcium nkag. Raws li tus xa xov tseem ceeb thib ob hauv cov hlwb, qhov nce hauv cov ntsiab lus ntawm calcium ions txuas ntxiv ua rau cov kab ke enzyme, xws li protein kinase C (PKC) thiab adenylate cyclase (AC). Kev ua kom cov adenylate cyclase catalyzes hloov pauv ntawm adenosine triphosphate (ATP) mus rau cyclic adenosine monophosphate (cAMP), uas ua haujlwm ua lwm tus neeg xa xov tseem ceeb thib ob thiab tuaj yeem qhib cov protein kinase A (PKA). Kev ua haujlwm ntawm PKA phosphorylates ib qho ntawm cov kev hloov pauv hauv qab thiab cov proteins, thaum kawg txhawb kev hloov pauv thiab txhais cov txheej txheem ntawm GH noob, yog li txhawb kev tso tawm ntawm GH los ntawm lub caj pas anterior pituitary thiab tsim lub cev pulsatile secretion qauv.
Qhov no pulsed secretion hom muaj qhov tshwj xeeb zoo. Tsis zoo li exogenous HGH, nws tsis ncaj qha ntxiv GH rau hauv lub cev, tab sis ua haujlwm los ntawm kev txhim kho lub caj pas pituitary lub peev xwm los zais GH. Thaum cov tshuaj hormones exogenous tau siv rau lub sijhawm ntev, lub cev maj mam txhim kho kev ua siab ntev rau cov tshuaj hormones, ua rau txo qis receptor rhiab heev. Nws yog ib qho tsim nyog yuav tsum tau nce ntxiv kom tau txais cov txiaj ntsig zoo ib yam, thiab tseem tuaj yeem ua rau muaj kev phiv xws li mob pob qij txha, edema, thiab ntshav qab zib siab. Lub amplitude thiab zaus ntawm induced GH pulses yog ze rau lub ntuj physiological lub xeev, uas muaj peev xwm ua tau zoo nyob rau hauv kev ruaj ntseg ntawm lub cev nyob rau hauv ib puag ncig thiab zam qhov teeb meem ntawm txo receptor rhiab heev los ntawm ntev - siv cov tshuaj hormones exogenous. Kev tshawb fawb tau pom tias nyob rau hauv tib lub voj voog kev kho mob, GH tso tawm los ntawm gonadorel tseem nyob hauv lub cev hloov pauv thiab lub cev hloov tau zoo rau nws, nrog qhov tshwm sim tsawg dua ntawm cov kev mob tshwm sim piv rau exogenous GH.
Tsis tas li ntawd, nws cov bioavailability yog qhov zoo dua li cov qauv ntawm qhov ncauj (xws li MK-677). Cov tshuaj hauv qhov ncauj tuaj yeem cuam tshuam los ntawm ntau yam xws li gastric acid thiab digestive enzymes thaum dhau los ntawm txoj hnyuv, ua rau cov tshuaj degradation thiab malabsorption. Thiab cov khoom no feem ntau yog siv los ntawm kev txhaj tshuaj lossis kev tswj qhov ntswg, uas tuaj yeem hla thawj qhov kev cuam tshuam ntawm lub plab zom mov thiab nkag mus rau hauv cov hlab ntsha ncaj qha, yog li txhim kho bioavailability ntawm cov tshuaj thiab ua kom nws muaj txiaj ntsig zoo rau GH secretion.
1. Kev tswj hwm metabolic
Ua si ntau lub luag haujlwm hauv kev tswj hwm cov metabolism, ua rau muaj kev cuam tshuam dual ntawm "nce nqaij thiab txo cov rog". Hais txog cov roj metabolism, nws tuaj yeem ua rau - adrenergic receptors ntawm adipocytes, txhawb lipolysis. Cov txheej txheem no zoo ib yam li cov rog rog tau pib los ntawm lub cev thaum lub sijhawm ua haujlwm lossis kev tshaib kev nqhis. Los ntawm kev ua kom cov enzymes xws li HSL, triglycerides khaws cia hauv adipocytes tau tawg ua cov rog dawb thiab glycerol, uas nkag mus rau hauv cov hlab ntsha thiab muab lub zog rau lub cev. Kev sim cov ntaub ntawv qhia tau hais tias kev siv tas li rau 8 lub lis piam tuaj yeem txo cov rog hauv lub cev los ntawm 6.8%. Hauv kev tshawb fawb soj ntsuam tsom rau cov neeg rog rog, cov neeg koom tsis tsuas yog poob qhov hnyav heev, tab sis kuj txhim kho kev faib tawm ntawm lub cev rog, tshwj xeeb tshaj yog cov rog hauv plab, ua ke nrog kev tswj hwm kev noj zaub mov kom tsim nyog thiab kev tawm dag zog thaum siv kev kho mob, uas txo qis kev pheej hmoo ntawm kev rog rog ntsig txog kab mob plawv, ntshav qab zib thiab lwm yam kab mob.
Nyob rau hauv cov nqe lus ntawm protein synthesis, indirectly txhawb protein synthesis (Anabolism) los ntawm stimulating lub secretion ntawm GH. GH tuaj yeem txhim kho kev thauj mus los thiab nce ntawm cov amino acids, ua kom cov ribosomes thiab cov khoom siv hloov pauv, txhawb cov protein synthesis hauv cov leeg hlwb, thaum inhibiting protein ntau. Qhov no ua rau cov leeg nqaij kom loj hlob thiab kho kom zoo dua qub, ua kom lub cev hnyav ntxiv. Hauv qhov kev sim saum toj no, cov neeg koom nrog nce lawv lub cev lean los ntawm 4.2% tom qab sivGHRP-2 ntsiav tshuajrau 8 lub lis piam, manifested raws li ib tug nce nyob rau hauv cov leeg ncig thiab cov leeg lub zog. Qhov no yog qhov tseem ceeb heev rau cov neeg ncaws pob, cov neeg nyiam kev tawm dag zog, thiab cov neeg uas raug kev txom nyem los ntawm cov leeg nqaij atrophy vim muaj mob lossis kev laus.
Tsis tas li ntawd, nws kuj inhibits kev siv cov piam thaj. Nws yuav txo cov uptake thiab oxidation ntawm qabzib los ntawm cov leeg thiab cov ntaub so ntswg adipose, ua rau cov ntshav qab zib nce mus rau ib qho twg. Cov txheej txheem ntawm kev ua haujlwm no pab txhawb nqa lub zog txaus rau lub cev thaum lub sijhawm muaj rog thiab cov protein synthesis, thaum zam kev tsis zoo ntawm cov ntshav qab zib hauv lub cev. Txawm li cas los xij, rau cov neeg mob ntshav qab zib lossis cov neeg uas tswj cov ntshav qabzib tsis zoo, nws yog qhov yuav tsum tau ua tib zoo saib xyuas cov ntshav qabzib thiab kho cov tshuaj hypoglycemic kom tsis txhob muaj qhov hloov pauv hauv cov ntshav qabzib ntau dhau.
2. Tiv thaiv kev mob thiab kho
Inflammation yog ib qho kev tiv thaiv ntawm lub cev rau stimuli xws li raug mob thiab kis kab mob, tab sis ntau o tuaj yeem ua rau cov ntaub so ntswg puas thiab ua haujlwm tsis zoo. Gonadorel muaj cov tshuaj tiv thaiv tseem ceeb - cov teebmeem inflammatory thiab muaj peev xwm siv tus nqi hauv kev kho mob ntawm cov kab mob xws li mob caj dab. Hauv cov qauv nas ntawm kev mob caj dab, cov kws tshawb fawb pom tias Gonadorel tuaj yeem txo cov tsos mob ntawm ntau txoj hauv kev.
Ntawm qhov tod tes, nws tuaj yeem txo cov qib ntawm inflammatory cytokine interleukin -6 (IL-6) hauv cov ntshav. IL-6 yog ib qho tseem ceeb pro-inflammatory cytokine uas ua lub luag haujlwm tseem ceeb hauv cov kab mob ntawm kev mob caj dab. Nws tuaj yeem qhib lub cev tiv thaiv kab mob, txhawb kev tso tawm ntawm cov kab mob sib kis, thiab ua rau mob pob qij txha thiab raug mob. Cov txiaj ntsig kev sim tau pom tias tom qab kev kho mob nrog Gonadorel, qib IL-6 hauv cov nas txo qis los ntawm 13.42 ± 0.47 txog 10.4 ± 0.8 (P<0.01), significantly inhibiting the progression of inflammatory response.
Ntawm qhov tod tes, nws kuj tuaj yeem txo qhov sib koom ua ke. Kev sib koom tes o yog ib qho ntawm cov tsos mob ntawm kev mob caj dab, feem ntau tshwm sim los ntawm o ua rau muaj zog exudate nyob rau hauv cov kab noj hniav sib koom ua ke thiab o ntawm cov ntaub so ntswg ib puag ncig. Los ntawm inhibiting qhov kev tso tawm ntawm inflammatory mediators thiab nce vascular permeability, cov kua dej nyob rau hauv lub sib koom kab noj hniav yog txo, li no txo cov℃ntawm kev sib koom o. Tsis tas li ntawd, nws cov txheej txheem yuav cuam tshuam nrog inhibition ntawm macrophage tso tawm nitrite / nitrate. Macrophages yog cov tshuaj tiv thaiv kab mob tseem ceeb hauv cov lus teb inflammatory, uas tso tawm ntau cov tshuaj nitrogen reactive xws li nitrite / nitrate thaum stimulation. Cov tshuaj no yog cytotoxic thiab tuaj yeem ua rau cov ntaub so ntswg puas tsuaj ntxiv. Nws tuaj yeem tswj hwm kev ua haujlwm ntawm macrophages, inhibit lawv qhov tso tawm ntawm nitrite / nitrate, yog li tiv thaiv cov ntaub so ntswg los ntawm kev puas tsuaj ntxiv, txhawb kev kho kev sib koom tes thiab kev ua haujlwm zoo.
3. Kev cai noj qab haus huv
Kev tswj kev noj qab haus huv yog ib txoj hauv kev ua kom lub cev muaj zog uas tswj hwm los ntawm ntau yam tshuaj hormones thiab neural signals. Los ntawm kev ua kom lub ghrelin receptor, qab los noj mov tuaj yeem txhim kho tau zoo. GHH yog peptide hormone secreted los ntawm gastric mucosa, hu ua "kev tshaib kev nqhis hormone". Nws tuaj yeem ua rau kev noj qab haus huv chaw tswj hwm ntawm hypothalamus, txhawb kev qab los noj mov, thiab nce kev noj zaub mov. Tom qab khi rau ghrelin receptor, cov nyhuv ntawm ghrelin tau simulated, ua rau muaj kev noj qab haus huv los txhim kho txoj hauv kev.
Kev tshawb fawb tau pom tias tom qab sivGHRP-2 ntsiav tshuaj, cov neeg koom nrog cov calorie ntau ntau txhua hnub tau nce 15% -20%. Cov yam ntxwv no ua rau nws yog ib qho cuab yeej pabcuam tseem ceeb thaum lub sijhawm cov leeg tsim. Rau cov neeg ncaws pob thiab cov neeg nyiam kev tawm dag zog, nws yog ib qho tsim nyog yuav tsum tau noj cov calories thiab cov protein kom txaus thaum lub sij hawm tsim cov leeg nqaij los txhawb cov leeg kev loj hlob thiab kho. Txawm li cas los xij, vim muaj kev cob qhia siab thiab kev tswj hwm kev noj zaub mov nruj, ntau tus neeg feem ntau xav tias tsis qab los noj mov thiab pom tias nws nyuaj kom ua tiav cov calorie kom tsawg. Kev siv nws tuaj yeem daws qhov teeb meem no tau zoo thiab pab lawv nce lawv cov khoom noj thaum lub sijhawm tsim cov leeg nqaij, tshwj xeeb tshaj yog cov khoom noj muaj protein ntau, txhawm rau ua kom tau raws li kev noj haus zoo ntawm cov leeg nqaij thiab txhim kho cov leeg nqaij.
4. Pw tsaug zog optimization
Kev pw tsaug zog yog lub sijhawm tseem ceeb rau lub cev rov qab los thiab kho, ua lub luag haujlwm tseem ceeb hauv kev loj hlob thiab kev loj hlob, kev tiv thaiv kab mob, kev tswj cov metabolism, thiab lwm yam. Kev zais ntawm GH muaj feem cuam tshuam nrog kev pw tsaug zog, tshwj xeeb tshaj yog thaum lub sijhawm pw tsaug zog uas GH secretion mus txog qhov kawg. Gonadorel tuaj yeem ua kom zoo rau kev pw tsaug zog zoo thiab txhim kho cov synchronization ntawm GH pulses thiab qeeb yoj pw.
Txoj kev tshawb nrhiav pom tias tom qab siv, cov neeg koom nrog lub sijhawm pw tsaug zog tau nce 25%. Hauv kev pw tsaug zog sib sib zog nqus, lub cev muaj ntau yam kev ua haujlwm ntawm lub cev tau so thiab rov qab los, thiab kev tso tawm ntawm GH kuj muaj zog dua, uas pab txhawb cov leeg nqaij, kho cov ntaub so ntswg puas, txhim kho kev tiv thaiv kab mob, thiab lwm yam. Rau cov neeg ncaws pob, kev pw tsaug zog zoo tuaj yeem ua kom rov qab qoj ib ce, txo qhov tshwm sim ntawm kev raug mob kis las, thiab txhim kho kev ua kis las. Rau cov neeg laus, kev txhim kho kev pw tsaug zog zoo tuaj yeem txo lub cev qaug zog, txhim kho lub neej zoo, thiab ncua kev laus. Tsis tas li ntawd, lub luag hauj lwm ntawm gonadorel hauv optimizing pw tsaug zog kuj tseem muaj feem xyuam rau nws cov kev cai ntawm neurotransmitters thiab neuroendocrine system. Nws tuaj yeem tswj hwm qib ntawm cov neurotransmitters xws li serotonin thiab dopamine hauv lub hlwb, txhim kho kev xav, thiab txhawb kev pw tsaug zog ruaj khov thiab sib sib zog nqus.
Cov yam ntxwv thiab kev txwv
Txawm hais tias daim ntawv qub yog kev txhaj tshuaj, cov ntsiav tshuaj daim ntawv ntawm cov khoom thov kom ua tiav cov txiaj ntsig zoo sib xws los ntawm kev tswj hwm qhov ncauj. Txawm li cas los xij, nws daim ntawv thov siv tau yuav tsum tau saib xyuas cov teeb meem tseem ceeb hauv qab no:
Lub bioavailability ntawm kev tswj qhov ncauj yog tsawg heev (0.3% -1%), feem ntau yog vim plab hnyuv enzyme degradation thiab daim siab ua ntej dhau los. Txawm hais tias bioavailability ntawm kev tswj qhov ntswg yog qhov siab (kwv yees li 53%), daim ntawv ntsiav tshuaj yog qhov nyuaj rau kev kov yeej qhov kev txwv no. Tam sim no, tsis muaj kev tshawb fawb loj loj los lees paub qhov ua tau zoo ntawm cov ntsiav tshuaj ntawm qhov ncauj.
Ib nrab-lub neej hauv cov ntshav yog li 30 feeb, thiab cov ntsiav tshuaj yuav tsum muaj cov txheej txheem tshwj xeeb (xws li microencapsulation thiab enteric txheej) txhawm rau ncua sijhawm tso tawm. Txawm li cas los xij, cov txheej txheem zoo li no yuav ua rau cov nqi nce ntxiv thiab cuam tshuam rau kev ruaj ntseg ntawm cov khoom xyaw nquag.
GHRP-2 ntsiav tshuajHauv kev lag luam grey feem ntau yog muag raws li lub npe ntawm "kev loj hlob hormone tso tawm peptide", nrog rau cov kev qhia tshwj xeeb xws li 5mg-10mg / lub raj mis, tab sis tsis muaj kev tswj hwm nruj. Qee cov khoom yuav muaj cov khoom xyaw uas tsis muaj cim, ua rau muaj kev phom sij.
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