Gonadotropin-ukukhupha hormone (GnRH): ingakumbi iziyobisi analogs

Gonadotropin-ukukhupha hormone (GnRH) yaziwa njenge hormone emoyeni luteinizing ihomoni (LHRH) kwaye lyuliberin nto leyo peptide ihomoni trophic linoxanduva ngokukhululwa FSH (follicle ekuvuseleleni hormone), kunye (LH), luteinizing hormone ukusuka yebhinqa sobuKristu. GnRH - hormone kuhlanganiswa yakhululwa ngxenye ka GnRH luvo. Le peptide bobabo kwintsapho gonadotropin-yokukhulula hormone kunye emele inkqubo osinachalny step hypothalamic-yebhinqa-adrenal. Eli phepha aya bachasene incindi yedlala gonadotropin-lokukhululwa.

isakhiwo

KaNobel, uAndrew V. Schally kunye Rozhe Giymen wachaza 1977 ekuqapheleni iimpawu GnRH: piroGlyu-Giese-yexeshana-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2. Yintoni kuxhaphakile ntetho peptides, ukulandelelana anikwe ukusuka N-terminus ku C-terminus ngenxa peptide ntetho, njengesiqhelo, kodwa umgangatho skip chirality uphawulo, exela ukuba acid kwi L-imilo ise. Nezishunqulelo angentla acid proteinogenic eqhelekileyo. An Okungumahluko piroGlyu - pyroglutamic acid, yemvelaphi glutamic acid. Kwi-C-terminus NH2 ibonisa ukuba chain iphela karboksidaminom endaweni carboxylate free.

yokuqaphela

Siphu- gonadotropin-yokukhulula hormone gene GNRH1 ibekwe chromosome 8 8. decapeptide Eqhelekileyo mammalian kuhlanganiswa 92 acid acid kwangaphambili-prohormone in yobuchopho phambi preoptic. Kuba ithagethi iindlela inkqubo eyahlukileyo elawula umgca hypothalamic-yebhinqa-adrenal elinganeno ngokwandisa amanqanaba estrogen emzimbeni.

ukusebenza

Gonadotropin-ukukhupha hormone secreted egazini nokuqukuqela portal vein kummandla yebhinqa ukuvelela udibaniso. GnRH ikhutshelwa igazi yebhinqa nokuqukuqela vein Portal equlathe iiseli gonadotropic apho receptors eyakho isebenze GnRH receptor ihomoni gonadotropin-ukundikhulula, receptors transmembrane ezisixhenxe conjugated ne G-protein zivuse beta isoform phosphoinositide phospholipase C, bekuza ku ekubsndakanyeni protein kinase C kunye calcium . Oku kukhokelela kokuba uqalile okanye ipoti ye ziiproteni aqukiweyo secretion kunye Yindibanisela gonadotropins FSH kunye LH. Ngexesha proteolysis GnRH yahlula ukuba imizuzu embalwa. Esengumntwana, umsebenzi yayo liphantsi kakhulu, nikhulela elivisayo okanye lokufikisa. Impumelelo ixhomekeke umsebenzi umsebenzi pulsatility enzala ilawulwa nzulu yi loop ingxelo. Kodwa umsebenzi GnRH ngexesha lokukhulelwa kungekho mfuneko. Isifo okanye nokuphazamiseka, kwakunye organic umonakalo uhlobo ukwenzakala yobuchopho kunye nangezilonda yebhinqa kunokubangela umsebenzi pulsatility olungafunekiyo. Amanqanaba prolactin iphakamileyo unciphisa umsebenzi GnRH, hyperinsulinemia kwaye liphuma kwaye ibangela kuphazamisa umsebenzi FSH kunye LH, ezinje zamaqanda polycystic. Kallmana syndrome luphawulwa yokungabikho GnRH yokuqaphela.

neurohormones

GnRH kunganxulunyaniswa kwi neurohormones. Iveliswe hormone gonadotropin-ukukhulula kule ndawo preoptic equka uninzi luvo GnRH-secreting. Ezi luvo asuka ancedisana ngeempumlo uze abeza kweli nobuchopho apho ekudibaneni medial uze iphaphatheke le ngxenye edibene luvo elide, ngaphezu kwe-1 mm ubude. Ungqamaniso GnRH ndimkhulule zibe zizithungu ezimbaxa kunceda ukuvelisa amagalelo eyodwa zobuchopho. Usebenzisa iqela zidlulisele ezahlukeneyo ezifana Gaba, glutamate kunye norepinephrine kulawulwa GnRH luvo secreting. Narpimer, emva ulawulo dlala-estrogen abafazi dopamine lukwakhuthaza ukukhululwa LH; kunye nabafazi ovariectomized dopamine kunganqanda ukukhululwa LH. Umlawuli ibalulekileyo yokukhululwa GnRH Kiss-peptin kwakhona kulawulwa yi estrogen. Noko ke, kwakukho ubukho secreting neuronal Kiss-peptin nokuvakalisa alpha kunye estrogen receptor.

Kubalulekile ukwazi ukuba yintoni na agonists incindi yedlala gonadotropin-lokukhululwa. Eli nqaku liza kuba ulwazi malunga nayo.

Impembelelo kwamanye amalungu

Indima GnRH kakuhle izifundo kwiinkqubo zobomi ukongeza ingqondo yebhinqa kunye ngxenye. Kukho kungenzeka ukuba onesiphumo kwi kwamadlala ngesondo kunye ngumkhaya kwakhona receptors GnRH kunye GnRH ngokwayo eziye zafunyanwa iiseli umhlaza, ovarian, endometrial, yesinye, wamabele.

Effects on ukuziphatha

Ukuziphatha ngokuveliswa hormone GnRH kananjalo ochaphazelekayo. Usapho lweentlanzi cichlid iintlanzi ebonisa igunya loluntu, babona ngcono ulawulo GnRH secretion, xa cichlids ezibuthathaka ekuhlaleni kufuneka ukuba kubekho ulawulo GnRH secretion. Ubungakanani luvo ukuba cell GnRH kuxhomekeke ukuziphatha nommandla ongqongileyo kwezentlalo. amaduna Okuninzi ehlukanisiwe ubungakanani enkulu secreting GnRH luvo ches abudala ilolo kangako. iimazi nokuzalana nawo imali encinane luvo ngakumbi iimazi iqela lolawulo. Ithetha ulawulo loluntu GnRH hormone.

Agonists incindi yedlala gonadotropin-yokukhupha kuxoxwa ngezantsi.

izicelo Medical

Kuba unyango abantu abagulayo phambi kokuba emiselweyo GnRH yendalo njengoko gonadorelin hydrochloride (Faktrel) kunye gonadorelin diatsetattetragidrata (Tsistorelin). isakhiwo yokuphila GnRH dekapiptida kukhokelele ekuyilweni unique, ushukumisa okanye abathintela gonadotropins ukuze uyolule isiqingatha-ubomi. Kwaye ezi analogs zokwenziwa of hormone zendalo indawo. Leuprorelin analog esetyenziswa ukunyanga endometriosis, kartsiomy ibele, wesinye kartsiomy kananjalo emveni kweminyaka ethile yophando ngo-1980, xa Vol. H. Komita olwenziwe nguGqirha Florence weYunivesithi Yale, ukunyanga lokufikisa kom, ibe nokubandakanywa oluqhubekayo.

Gonadotropin-ukukhupha hormone: ixabiso

I-avareji yeendleko webhotile nganye - evela engange 300.

Ukuziphatha Animal Ezocansi

Iiyantlukwano nabo kubangelwa umsebenzi ukuziphatha ngokwesondo GnRH. Umzekelo, umboniso oluphuculweyo ukuziphatha ngokwesini ababhinqileyo kubangela ukwanda kwinqanaba GnRH. In ndlunkulu emhlophe-sithsaba ukwanda kwemfuno ithe yancola emva kokuba ukuqaliswa GnRH, kwaye oluphuculweyo ezincancisayo umboniso yokuziphatha iimazi, leyo ukubonwa kwi shrew elide-ezinomsila emhlophe-unamazinyo kwaye ixesha layo abagxothwa ukuhla ngexesha umboniso emva inkunzi intshukumo kwicala yakhe ngumsila wena. It kwandisa umsebenzi amadoda testosterone kunyuke nge GnRH ngaphezu kwinqanaba eliqhelekileyo lomsebenzi testosterone. umsebenzi ukonakala GnRH ibangela isiphumo amalungu aversive yokuzala kunye nokuziphatha koomama. Xa sithelekisa neempuku nemazi ngexesha inkqubo eqhelekileyo GnRH, iimazi banenkxalabo ngakumbi mva kunokuba kubekho inani eliphunguliweyo luvo yi-30%. Kungenzeka, ezi iimpuku kukushiya alimele ngokwahlukileyo, nto leyo a elide sazifumana zona.

izicelo Veterinary

Apho kuyimfuneko gonadotropin-ukukhulula hormone? Amachiza asetyenziswa amayeza lwezilwanyana njengeyeza yonyango lwesifo esinganyangekiyo ovarian ezinkomeni. A Togu zokwenziwa kwayo, deslorelin ezisetyenziselwa ulawulo lwemfuyo imisebenzi ekuzaleni usebenzisa zikhule nokuqulunqa ukukhululwa ezinzileyo.

Cinga analogue incindi yedlala gonadotropin-lokukhululwa.

Agonists kunye abamelene incindi yedlala gonadotropin-ukukhulula

Ngokwahlukeneyo, iqela neziyobisi mechanism impembelelo linokubizwa ngokuba i agonist incindi yedlala gonadotropin-lokukhululwa. Oku kuthetha ukuba isiphumo eli qela iziyobisi ingqondo yebhinqa ibangela isiphumo efana kwesiphumo hormone yayo. Abameli beli qela ingabizwa "Sinarel", "Lyukrin Gonapeptil yokugcina." Le agonist incindi yedlala gonadotropin-lokukhululwa. Le imixube isebenze ngaphambi nasemva unyango fibroids, endometriosis naphambi intsumpa kokususa isibeleko (hysterectomy) kwi unyango ukungachumi. izinto Active phantsi kwempembelelo lekhefu juice esiswini yaye ke ngoko zonke amachiza ngokuzitofela phantsi kwesikhumba okanye kungena interanazolno kwezihlunu.

Ngu abamelene hormone gonadotropin-ekhulula ezi "Tsetrotid" ( "Tsetroteriks"), "ganirelix" njalo njalo.