Ghrp-2 10 mg

▎ GHRP-2 Structure

Source: PubChem

Sequence: AXAWFK Molecular Formula: C 45H 55N 9O6 Molecular Luj: 817.98 g/mol CAS Nr .: 158861-67-7 PubChem CID: 6918245 Cov ntsiab lus: Pralmorelin; pralmorelina; KP-102; pralmoreline

▎ GHRP-2  Kev Tshawb Fawb

Kev tshawb fawb keeb kwm ntawm GHRP-2 yog dab tsi?

Kev loj hlob hormone plays lub luag haujlwm tseem ceeb hauv tib neeg txoj kev loj hlob, kev loj hlob, thiab kev sib npaug ntawm metabolic. Cov kws tshawb fawb tau ntev nrhiav cov tshuaj uas muaj peev xwm tswj tau nws qhov zais cia. Kev loj hlob hormone-tso peptides (GHRPs), ib chav kawm ntawm hluavtaws oligopeptides uas txhawb kev loj hlob hormone tso tawm, tau tshwm sim los ntawm kev tshawb fawb.

GHRP-2 ua raws li qhov kev txiav txim ntawm ghrelin los ntawm kev khi rau ghrelin receptor, ua kom pom cov kev taw qhia kom ua tau zoo txhawb GH tso tawm. Nws qhia tau hais tias muaj peev xwm hauv kev kuaj mob thiab kho kev loj hlob hormone tsis txaus, cuam tshuam hauv anorexia, thiab tiv thaiv lub cev puas tsuaj, tsav kev tshawb fawb tob rau hauv nws cov txheej txheem thiab kev siv.

Dab tsi yog qhov txheej txheem ntawm kev txiav txim rau GHRP-2?

Txoj Cai Loj Hlob Hormone Secretion

Ua ntawm Hypothalamic-Pituitary Axis:

GHRP-2 txhawb nqa kev loj hlob hormone (GH) tso tawm los ntawm kev ua haujlwm tshwj xeeb dual-complementary tsom rau ob qho tib si hypothalamus thiab pituitary caj pas (Bowers CY). Hauv qib pituitary, GHRP-2 khi rau kev loj hlob hormone-tso cov tshuaj hormone receptor (GHS-R). Raws li kev khi rau GHS-R, GHRP-2 pib ua ib qho kev cuam tshuam ntawm intracellular signaling txheej xwm. Piv txwv li, nws activates phospholipase C (PLC), uas catalyzes hydrolysis ntawm phosphatidylinositol-4,5-bisphosphate (PIP2) ntawm cell membrane rau inositol trisphosphate (IP3) thiab diacylglycerol (DAG). IP3 txhawb nqa calcium ion tso tawm los ntawm endoplasmic reticulum, thaum DAG activates protein kinase C (PKC), thaum kawg ua rau GH tso (Roh SG,). Hauv kev tshawb fawb siv bovine pituitary hlwb, GHRP-2 ntawm ntau qhov ntau (10⁻⊃1; ⊃3; mus rau 10⁻⁷ M) nce GH secretion (P <0.05), qhia qhov ncaj qha stimulatory nyhuv ntawm GHRP-2 ntawm GH secretion los ntawm pituitary hlwb ^[1].

Synergistic Action nrog Kev Loj Hlob Hormone-Tshuaj Hormone (GHRH):

GHRP-2 nthuav tawm kev sib koom ua ke nrog GHRH hauv kev txhawb nqa GH tso tawm. Thaum sib koom ua ke rau cov hlwb pituitary, lawv ua los ntawm cov kev taw qhia sib txawv uas thaum kawg sib koom ua ke los txhawb GH secretion. Cov kev tshawb fawb qhia tias GHRH feem ntau ua rau adenylate cyclase (AC), nce intracellular cAMP qib kom ua rau cov protein kinase A (PKA), yog li txhawb nqa GH gene transcription thiab GH synthesis / tso tawm. Hloov pauv, GHRP-2 siv nws cov teebmeem ntawm PLC-IP3 / DAG-PKC txoj hauv kev tau piav qhia saum toj no. Lawv cov kev sib koom ua ke ua rau muaj kev cuam tshuam ntau ntxiv GH tso tawm. Hauv kev sim yaj pituitary cell, ob qho tib si GHRH (10 nM) thiab GHRP-2 (100 nM) ib tus zuj zus nce GH mRNA qib thiab GH tso tawm nyob rau lub sijhawm nyob ntawm 0.5-2 teev; Cov nyhuv no tau ua kom zoo dua thaum ua ke ^[2].

Txoj Cai Kev Loj Hlob Hormone Secretion:

GHRP-2 txhawb nqa kev loj hlob hormone (GH) tso tawm los ntawm qhov tshwj xeeb dual-complementary nkaus, ib txhij tsom mus rau hypothalamus thiab pituitary caj pas (Bowers CY). Hauv qib pituitary, GHRP-2 khi rau kev loj hlob hormone-tso cov tshuaj hormone receptor (GHS-R). Raws li kev khi rau GHS-R, GHRP-2 pib ua ib qho kev cuam tshuam ntawm intracellular signaling txheej xwm. Piv txwv li, nws activates phospholipase C (PLC), uas catalyzes hydrolysis ntawm phosphatidylinositol 4,5-bisphosphate (PIP2) ntawm lub cell membrane rau hauv inositol trisphosphate (IP3) thiab diacylglycerol (DAG). IP3 txhawb nqa calcium ion tso tawm los ntawm endoplasmic reticulum, thaum DAG activates protein kinase C (PKC), thaum kawg ua rau GH tso (Roh SG,). Hauv kev tshawb fawb siv bovine pituitary hlwb, GHRP-2 ntawm ntau qhov ntau (10⁻⊃1; ⊃3; mus rau 10⁻⁷ M) nce GH secretion (P <0.05), qhia qhov ncaj qha stimulatory nyhuv ntawm GHRP-2 ntawm GH secretion los ntawm pituitary hlwb ^[1].

Kev kho mob ntawm Anorexia:

Rau cov neeg mob anorexia, intranasal tswj ntawm GHRP-2 nce kev tshaib kev nqhis thiab noj zaub mov, txo qis satiety thaum ntxov, thiab txhim kho cov tsos mob hypoglycemia. Tom qab 14 lub hlis ntawm kev tswj hwm GHRP-2, cov neeg mob maj mam nce 6.7 kg hauv lub cev hnyav. Cov txheej txheem tuaj yeem koom nrog GHRP-2 ua tus ghrelin receptor agonist los ua cov teebmeem ntawm ghrelin, yog li hloov kho lub qab los noj mov thiab txhim kho cov neeg mob noj tus cwj pwm thiab noj zaub mov zoo ^[3].

Daim duab 1 (A) Kev hloov pauv hauv lub cev hnyav, cov leeg nqaij, thiab rog rog tom qab kho nrog kev loj hlob hormone tso tawm peptide-2 (GHRP-2). Cov rog thiab cov nqaij pob txha raug soj ntsuam siv txoj kev bio-impedance. Txhua qhov ntsuas tau maj mam nce ntxiv, nrog rau lub cev hnyav thiab kev siv zog txhua hnub nce los ntawm -1.5 mus rau 2.4 kg thiab 12% mus rau 36%, feem, tom qab ghrelin infusion. (B) Kev hloov pauv hauv kev loj hlob hormone (GH) thiab insulin-zoo li kev loj hlob yam 1 (IGF-1) qib tom qab kho GHRP-2. GH poob thaum IGF-1 nce tom qab 12 lub hlis. (C) Kev hloov pauv hauv kev noj zaub mov zoo. Retinol binding protein (RBP) thiab tag nrho cov protein (TP) tau nce sai, nrog albumin (Alb) nce tom qab 4 lub hlis. Cov kev txwv no tau nce ntxiv tom qab 12 lub hlis. (D) Kev hloov pauv hauv acyl ghrelin (AG) thiab des-acyl ghrelin (DAG) qib tom qab GHRP-2 tswj hwm. Kev yoo mov DAG thiab AG tau nce, thiab DAG / AG piv tau txo qis tom qab 10 lub hlis. BW; lub cev hnyav.

Source: PubMed ^[3]

Daim ntawv thov kev kho mob ntawm GHRP-2 yog dab tsi?

Kev kuaj mob ntawm kev loj hlob hormone secretion deficiency: GHRP-2 yog tshuaj siv los ua tus neeg saib xyuas kev loj hlob hormone deficiency. Rau cov neeg laus txoj kev loj hlob hormone tsis txaus, qhov kev ntsuam xyuas thoob ntiaj teb thawj kab kev kuaj mob yog cov tshuaj insulin tolerance test (ITT). Txawm li cas los xij, vim nws muaj peev xwm ua rau muaj qhov tshwm sim tsis zoo, nws yog contraindicated rau qee tus neeg mob. Cov kev tshawb fawb tau npaj siv GHRP-2 los kuaj xyuas cov neeg laus loj hlob hormone deficiency (GHD). Txoj kev tshawb no cuv npe kawm 77 tus neeg noj qab haus huv thiab 58 tus neeg mob siab tshaj GH <3 μg / L raws li kev txiav txim los ntawm ITT. Txhua tus neeg tau txais kev txhaj tshuaj ntawm 100 μg GHRP-2, ua raws li kev kuaj ntshav tom qab 2 teev. GH qib tau ntsuas los ntawm kev ntsuas immunoradiometric. Cov txiaj ntsig tau pom tias txhua qhov kev kawm tau nthuav tawm cov ntshav siab GH hauv 60 feeb tom qab GHRP-2 kev tswj hwm. GH teb rau GHRP-2 tsis cuam tshuam los ntawm poj niam txiv neej. Txawm hais tias cov lus teb tau qis me ntsis hauv cov neeg laus thiab cov neeg rog rog, qhov no tsis cuam tshuam rau GHD kev kuaj mob. Rov ua dua kev ntsuam xyuas pom tau zoo rov ua dua ntawm txoj kev no. Thaum siv GHRP-2 los kuaj GHD, tus nqi txiav tawm ntawm 15 μg / L sib raug rau tus nqi kuaj mob ntawm 3 μg / L hauv ITT, qhia tias kev teeb tsa cov tshuaj tsim nyog GH concentration cutoff ntseeg tau kuaj xyuas qhov loj hlob hormone tsis txaus ^[4].

Kev kho mob ntawm Anorexia: Rau cov neeg mob uas muaj keeb kwm ntev ntawm anorexia, GHRP-2 tuaj yeem sawv cev rau tus neeg sawv cev kho mob. Ib txoj kev tshawb fawb tau tswj hwm GHRP-2 intranasally ua ntej txhua pluas noj rau ib xyoos rau tus neeg mob uas muaj 20 xyoo keeb kwm ntawm anorexia. Ua ntej kev kho mob, txawm hais tias tus neeg mob qhov kev ntshai ntawm kev noj zaub mov thiab xav kom nyias nyias tau ploj zuj zus los ntawm cov kev kho mob yav dhau los, kev ua haujlwm ntawm plab hnyuv tiv thaiv kev noj zaub mov ntau ntxiv thiab qhov hnyav nce. Cov tsos mob muaj xws li ntuav tom qab ntuav, cem quav, mob plab hnyuv, thiab hypoglycemia. Ua raws li kev tswj hwm GHRP-2, tus neeg mob tau ntsib kev tshaib kev nqhis thiab kev noj zaub mov ntau ntxiv, txo qis satiety thaum ntxov, cov tsos mob hypoglycemia zoo tuaj, thiab lub cev hnyav zuj zus ntxiv los ntawm 6.7 kg (los ntawm 21.1 kg txog 27.8 kg) hauv 14 lub hlis ntawm kev pib kho. Kev qaug zog thiab cov leeg muaj zog tuaj yeem txhim kho, kev ua haujlwm ntawm lub cev thiab lub hlwb tau nce, thiab tsis muaj kev phiv tseem ceeb tau pom nrog kev tswj hwm intranasal mus ntev. Qhov no qhia tias GHRP-2 yuav yog tus neeg sawv cev kho mob zoo rau cov neeg mob uas muaj mob hnyav heev ^[3].

Alleviating Burn-Induced Dysfunction: Tom qab kub hnyiab hnyav, nce cov tshuaj hormones catabolic thiab inflammatory cytokines nrog rau cov tshuaj hormones anabolic qis ua rau metabolic hyperactivity, txo qis lub cev nqaij daim tawv, thiab nqaij ntshiv. Txawm hais tias muaj ntau yam kev kho mob xws li kev tawm dag zog thiab kev siv cov tshuaj hormones anabolic (insulin, kev loj hlob hormone, IGF-I, lossis steroids) tau thov los yog ua haujlwm, lawv cov teebmeem tseem tsis zoo. Cov txiaj ntsig kev sim qhia tau hais tias qhov kev cais tawm tshiab los tiv thaiv cachexia peptide ghrelin txo qis hauv cov nas tom qab hlawv. Exogenous ghrelin tuaj yeem rov qab poob phaus los ntawm kev noj zaub mov ntau ntxiv thiab txhim kho cov leeg nqaij hauv nas. Nws kuj tseem txo cov nqaij pob txha protein degradation hauv cov nas hlawv los ntawm normalizing nqaij mRNA qhia ntawm E3 ubiquitin ligase, MuRF1, thiab MAFbx. Qhov luv luv ib nrab-lub neej ntawm ghrelin txwv nws daim ntawv thov kev kho mob. Nyob rau hauv sib piv, cov hluavtaws hexapeptide kev loj hlob hormone-tso peptide 2 (GHRP-2) yog ib tug ruaj khov thiab muaj zog GHRP receptor agonist uas ua rau kom lub cev hnyav nyob rau hauv nas, nthuav tawm los tiv thaiv cov kab mob hauv cov nas tsuag, thiab txhim kho catabolic metabolism hauv cov neeg mob hnyav. GHRP-2 muaj txiaj ntsig zoo rau lub cev qhov hnyav, noj zaub mov, thiab cov leeg nqaij pob txha tawg hauv cov nas hlawv, txo qis kev ua haujlwm tsis zoo [5].

Xaus

GHRP-2 activates kev loj hlob hormone secretion los ntawm stimulating cov teeb meem cuam tshuam txoj kev los ntawm nws cov kev ua ntawm GHS-R nyob rau hauv lub hypothalamic-pituitary axis. Kev kho mob, nws tuaj yeem kuaj xyuas qhov kev loj hlob hormone tsis txaus thiab kho cov mob xws li anorexia, septic mob raum raug mob, thiab tom qab hlawv tsis ua haujlwm, thaum tseem muaj cov teebmeem analgesic thiab antioxidant.

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

Haruta I yog ib tus kws kho mob-tus kws tshawb fawb koom nrog Lub Tsev Haujlwm Saib Xyuas Kev Noj Qab Haus Huv Psychosomatic Internal Medicine ntawm Kagoshima University's Graduate School of Medical and Dental Sciences hauv Nyij Pooj. Nws kev tshawb nrhiav kev txhais lus tsom mus rau endocrine thiab metabolic cuam tshuam hauv kev mob hnyav anorexia nervosa. Haruta kuv tau teev nyob rau hauv qhov kev siv ntawm cov ntaub ntawv pov thawj [3].

▎ Cov Lus Qhia Tseem Ceeb

[1] Roh SG, He ML, Matsunaga N, Hidaka S, Hidari H. Mechanisms of action of growth hormone-tso peptide-2 in bovine pituitary cells. Phau ntawv Journal of Animal Science 1997; 75(10): 2744-2748.DOI: 10.2527/1997.75102744x.

[2] Yan M, Hernandez M, Xu R, Chen C. Cov nyhuv ntawm GHRH thiab GHRP-2 kev kho mob hauv vitro ntawm GH secretion thiab qib ntawm GH, pituitary transcription factor-1, GHRH-receptor, GH-secretagogue-receptor thiab somatostatin receptor mRNAs hauv ovine pituitary hlwb. European Journal of Endocrinology 2004; 150(2): 235-242.DOI: 10.1530/eje.0.1500235.

[3] Haruta I, Fuku Y, Kinoshita K, et al. Ib xyoos intranasal daim ntawv thov ntawm kev loj hlob hormone tso tawm peptide-2 txhim kho lub cev hnyav thiab hypoglycemia nyob rau hauv tus neeg mob hnyav emaciated anorexia nervosa. Phau ntawv Journal of Cachexia Sarcopenia thiab Muscle 2015; 6(3): 237-241.DOI: 10.1002/jcsm.12028.

[4] Chihara K, Shimatsu A, Hizuka N, Tanaka T, Seino Y, Katofor Y. Kev kuaj mob yooj yim siv GH-tso peptide-2 hauv cov neeg laus GH tsis txaus. European Journal of Endocrinology 2007; 157(1): 19-27.DOI: 10.1530/EJE-07-0066.

[5] Balasubramaniam A, Joshi R, Phooj Ywg LA, James JH. GHRP-2 attenuates burn-induced dysfunctions nyob rau hauv nas. Kev nce qib hauv Kev sim tshuaj thiab Biology 2009; 611: 571-572.DOI: 10.1007/978-0-387-73657-0_251.

Tag nrho cov kab lus thiab cov ntaub ntawv ntawm cov khoom lag luam muab rau ntawm lub vev xaib no tsuas yog rau cov ntaub ntawv tshaj tawm kev tshaj tawm thiab cov hom phiaj kev kawm.  

Cov khoom muab rau hauv lub vev xaib no yog npaj tshwj xeeb rau kev tshawb fawb hauv vitro. Kev tshawb fawb hauv vitro (Latin: * hauv iav *, lub ntsiab lus hauv iav) yog ua los ntawm tib neeg lub cev. Cov khoom no tsis yog tshuaj, tsis tau txais kev pom zoo los ntawm US Food and Drug Administration (FDA), thiab yuav tsum tsis txhob siv los tiv thaiv, kho, lossis kho txhua yam mob, kab mob, lossis mob. Nws raug txwv nruj raws li txoj cai los qhia cov khoom no rau hauv tib neeg lossis tsiaj lub cev hauv txhua daim ntawv.