I. Khoom Keeb Kwm
Gonadorelin yog ib qho hluavtaws decapeptide nrog cov qauv zoo ib yam rau gonadotropin- tso cov tshuaj hormone (GnRH) ib txwm zais los ntawm hypothalamus. Nws txoj kev loj hlob yog raws li kev ua kom huv thiab kev tsom xam ntawm GnRH qauv los ntawm hypothalamus ntawm npua thiab yaj hauv 1971, uas Andrew Schally thiab Roger Guillemin tau txais 1977 Nobel nqi zog hauv Physiology lossis Tshuaj. Nws cov khoom siv hluavtaws tau ua tiav sai sai, thiab txij li xyoo 1970s, nws tau siv los ua ib qho ntawm GnRH analogs ntxov tshaj plaws hauv kev kho tsiaj thiab tib neeg kev kho mob thiab kev tshawb fawb.
II. Khoom Parameters
Amino acid sequence: pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂ (ib tsab ntawv: pEHWSY2GRPG)
• Molecular formula: C₅₅H₇₅N₁₇O₁₃
- Molecular hnyav: Kwv yees li 1182.3 Da
• CAS naj npawb: 33515-09-2 (free base); 34973-08-5 (acetate) CAS TSIS TAU.
• Cov tsos mob: Dawb los yog tawm -dawb lyophilized hmoov, hygroscopic, yooj yim soluble hauv dej
• Purity: Qib Kev Tshawb Fawb / Pharmacopoeia, feem ntau Ntau dua lossis sib npaug li 98% (HPLC)
- Solubility: Soluble nyob rau hauv sterile dej, dilute acetic acid, PBS, thiab lwm yam.; pom zoo kom khaws kev tiv thaiv los ntawm lub teeb kom khaws Trp/Tyr residues.
• Kev ruaj ntseg: qhuav hmoov -20℃Khaws rau hauv lub thawv ntim khoom tiv thaiv los ntawm lub teeb; Tom qab hloov kho, khaws cia ntawm 4℃rau lub sijhawm luv thiab -20℃rau lub sijhawm ntev. Aliquot kom tsis txhob rov qab khov-thaw mus.
III. Core Functions
Gonadorelin khi rau GnRH receptors ntawm anterior pituitary gonadotropic hlwb, stimulating synthesis thiab pulsatile tso tawm ntawm luteinizing hormone (LH) thiab follicle-stimulating hormone (FSH) ntawm Gq/11-PLC-IP3/DAG-Ca²⁺ teeb liab txoj kev. Qhov no tswj cov hypothalamic-pituitary-gonadal axis (HPG axis), kev sib deev hormone secretion, thiab gametogenesis.
Cov ntsiab lus tseem ceeb: Kev tswj hwm pulsatile tswj / txhawb LH / FSH secretion; tsis tu ncua tsis yog -pulsatile raug ua rau receptor downregulation thiab LH / FSH inhibition (qhov no yog lub hauv paus ntsiab lus tom qab siv qee qhov ntev - ua GnRH agonists rau kev kho kab mob, tab sis Gonadorelin nws tus kheej feem ntau siv rau "stimulation/replacement" es tsis yog inhibition).
IV. Core Zoo
• Zoo biocompatibility: Cov qauv zoo ib yam rau endogenous GnRH, nrog rau qhov zoo -txhais tau thiab kwv yees txoj hauv kev ntawm kev ua. • Cov nqi kuaj mob siab: tuaj yeem siv los ua GnRH stimulation test (feem ntau ib zaug 100 µg koob tshuaj rau cov neeg laus, IV/SC) los ntsuas pituitary teb los ntawm kev hloov pauv hauv LH/FSH.
• Pulse therapy friendly: Kev siv tshuaj sib quas ntus / mem tes tuaj yeem siv los kho lossis txhawb HPG axis ua haujlwm raws li cov lus qhia tshwj xeeb, tsis zoo li qee qhov ntev - ua yeeb yam analogs uas pib lub hom phiaj inhibition.
• Cov keeb kwm ntev ntawm kev siv: Diagnostic applications tau muaj txij li puag ncig xyoo 1980s (xws li Factrel), thiab tib neeg cov ntaub ntawv tshawb fawb kuj muaj ntau.
V. Siv tau Scenarios
• Kev kuaj mob: GnRH stimulation test los ntsuas pituitary gonadotropin muaj nuj nqi, hypothalamic{0}} cov kab mob pituitary, los yog kev ua haujlwm tom qab ua haujlwm (feem ntau suav nrog ntau cov ntshav kuaj ua ntej thiab tom qab txhaj tshuaj los ntsuas LH/FSH raws li txoj cai).
• Tib neeg Kev Kho Mob Muaj feem xyuam (Ib Cheeb Tsam / Kev Siv Keeb Kwm): Siv rau hypothalamic amenorrhea, infertility/ovulation induction cuam tshuam nrog hypogonadotropic hypogonadism, thiab lwm yam.
• Txiv neej-Cov Kev Tshawb Fawb Txog Kev Tshawb Fawb thiab Kev Sib Tham: Nyob rau hauv cov ntsiab lus ntawm kev kho testosterone (TRT), kev siv tshuaj sib quas ntus qee zaum siv los ua kom muaj cov cim qhia txog endogenous gonadotropic thiab cov qog nqaij hlav ua haujlwm (feem ntau yog rau kev tshawb fawb / kev sib tham ntawm tus kheej).
• Veterinary Applications: Ovulation induction nyob rau hauv nyuj, yaj, thiab lwm yam tsiaj nyeg; kev tswj ntawm zes qe menyuam cysts, thiab lwm yam. (ntau yam kev lag luam kws kho tsiaj formulations tau pom zoo thaum ntxov).
• Kev Tshawb Fawb: Kev tshawb fawb cov cuab yeej peptides rau HPG axis mechanisms, GnRH receptor pharmacology, gametogenesis, thiab kev tswj hwm poj niam txiv neej.
VI. Cov kev ceev faj
• Ib nrab luv heev-lub neej: Kev faib tawm ib nrab- lub neej yog kwv yees li ob peb feeb, lub davhlau ya nyob twg ib nrab-lub neej nyob hauv kaum feeb ntau; yog li ntawd, kev kuaj mob feem ntau siv ib qho kev txhaj tshuaj bolus; Kev kho mob feem ntau yuav tsum tau siv lub twj tso kua mis pulse los yog noj tsis tu ncua.
- Tshuaj- cuam tshuam txog qhov tshwm sim: qhov chaw txhaj tshuaj, mob taub hau, ua kom lub ntsej muag, xeev siab, thiab lwm yam, tej zaum yuav tshwm sim; Tsis tshua muaj kev tsis haum tshuaj / anaphylactoid cov tshuaj tiv thaiv yuav tsum tau saib xyuas.
• Cov xwm txheej tshwj xeeb: Nyob rau hauv cov ntsiab lus ntawm kev pab yug me nyuam, tej zaum yuav muaj kev pheej hmoo xws li zes qe menyuam hyperstimulation (OSH) (txog rau cov txheej txheem thiab tus kheej).
• Kev tswj hwm thiab kev txwv tsis pub siv: Hauv ntau thaj tsam, Gonadorelin yog daim ntawv xaj / tswj kev siv kho mob; kev tshawb fawb- cov khoom qib feem ntau yog txwv rau kev tshawb fawb hauv chav kuaj thiab tsis tas txhais tau tias lawv tuaj yeem siv ncaj qha rau tib neeg kev sim tshuaj; qee lub teb chaws / cheeb tsam yuav tsis muaj kev lag luam raws li tib neeg cov qauv.
- Kev tuav thiab khaws cia: Nws raug pom zoo kom tiv thaiv los ntawm lub teeb thiab noo noo, thiab tsis txhob rov khov dua -thaw cycles; tom qab rov tsim kho dua, khaws cia rau hauv cov xwm txheej siv tau rau luv / ntev- siv sijhawm.
VII. Dab Neeg Zoo
• Kev kuaj mob: GnRH stimulation test nrog ib zaug 100 µg IV / SC koob tshuaj rau cov neeg laus tau raug siv hauv kev kho mob los txiav txim siab pituitary gonadotropin muaj nuj nqi thiab cov lus teb nkhaus, thiab los pab rau kev ntsuam xyuas ntawm hypothalamic- kab mob pituitary.
- Kev Tshawb Fawb Txog Kev Kho Mob: Hauv cov poj niam hypothalamic amenorrhea/hypothalamic hypogonadotropic infertility, pulsatile kev tswj hwm ntawm cov twj tso kua mis portable (piv txwv li, 5–20 µg / pulse, 90–120 feeb intervals) kom induce/restore ovulation.
• Ntev-Lub Sijhawm Kev Tshawb Fawb Lub Sijhawm: Kev sib xyaw thiab muab tso rau hauv kev siv xyoo 1970, xyoo tom ntej no tau sau ntau cov ntaub ntawv tshawb fawb tib neeg thiab tsiaj, ua rau nws yog "tus qauv / kev xaiv" hauv HPG axis kev soj ntsuam thiab qee txoj hauv kev kho mob.
Tus nqi
Gonadorelin tus nqi tseem ceeb nyob hauv nws qhov tseeb "kev sojntsuam-raws li" lossis "physiologically hloov" hypothalamic signals siv cov molecule zoo ib yam nkaus rau endogenous GnRH- ua cov cuab yeej kuaj xyuas kom muaj nuj nqis pituitary tso zis thiab, raws li qhov tsim nyog rau kev hloov kho PG. Tsis tas li ntawd, vim nws qhov zoo - cov qauv tau hais tseg, lub sijhawm luv luv ntawm kev ua, thiab tus cwj pwm pulsatile meej, nws tau ntev tau siv los ua peptide tseem ceeb hauv kev tshawb fawb endocrine thiab kev loj hlob.
Cim npe nrov: High-purity peptide tshuaj Gonadorelin 2mg/vial, Tuam Tshoj High-purity peptide tshuaj Gonadorelin 2mg/vial manufacturers, lwm tus neeg, Hoobkas
