200124-22-7 Tert-butoxycarbonyl-arginine(Pbf)-OH

Boc-Arg (Pbf) -OH ndi chochokera ku arginine.
Bivalirudine, anticoagulant yopangidwa yomwe ndi msuweni wa 20-peptide wa hirudin, inavomerezedwa kuti igulitse ku United States mu 2000. Jekeseniyo ndi chinthu choyera, chotayirira kapena cholimba cha amorphous.Bivarudine ikhoza kumangirira mwachindunji ku malo othandizira a thrombin ndi malo omangiriza kunja kwa anion, ndikuletsa mwachindunji ntchito ya thrombin, motero kulepheretsa zomwe zimakhudzidwa ndi thrombin, ndipo zotsatira zake zimasinthidwa.Bivarudine amagwiritsidwa ntchito makamaka ngati anticoagulant for elective percutaneous coronary intervention (PCI) mwa akuluakulu.
Bivarudine ndi inhibitor yachindunji ya thrombin, yomwe imamangiriza makamaka malo othandizira ndi anion exo-binding sites of thrombin free and on thrombus.Njira yomangiriza pakati pa bivaludine ndi thrombin imatha kusinthika, ndipo thrombin imatha kubwezeretsa ntchito yachilengedwe ya thrombin mwa pang'onopang'ono enzymolysis ya chomangira cha peptide pakati pa bivaludine Arg3-Pro4.
Kafukufuku wa m'galasi wasonyeza kuti bivarudine osati ziletsa ofananira nawo ufulu thrombin, komanso ziletsa thrombin kumanga ndi magazi kuundana popanda neutralized ndi zinthu anamasulidwa ndi mapulateleti.Itha kutalikitsa nthawi ya prothrombin (APTT), nthawi ya thrombin (TT), nthawi ya prothrombin (PT) ndi nthawi yogwira ntchito ya coagulation (ACT) yoyendetsedwa ndi plasma wamba.Pali ubale wofananira ndi kuchuluka kwa bivarudine, koma ngati kulumikizanaku kulipo muzachipatala sikudziwika bwino.
Zanenedwa m'mabuku kuti ma pharmacokinetics a odwala omwe akukumana ndi percutaneous coronary angioplasty (PTCA) amakhala pamzere pambuyo pa intravenous makonzedwe a bivarudine.Wodwalayo anapatsidwa 1 mg / kg intravenously ngati mlingo wolemetsa, wotsatiridwa ndi kulowetsedwa wina wa IV wa 2.5 mg / kg / hr kwa maola 4, omwe adakhazikika pa 12.3 ± 1.7 mg / ml mu vivo.Bivarudine imachotsedwa ku plasma ndi aimpso hydrolysis ndi kuwonongeka kwa protease.The chilolezo theka moyo wa odwala yachibadwa aimpso ntchito za 25min, ndi chilolezo theka la moyo wa odwala zolimbitsa aimpso insufficiency ndi anawonjezera.Pafupifupi 25% ya bivarudine imatha kuchotsedwa ndi dialysis ndikuyeretsedwa ndi hemodialysis.ACT iyenera kuyang'aniridwa mwa odwala omwe ali ndi vuto laimpso.Mwa odzipereka athanzi, mphamvu ya anticoagulant idawonedwa pambuyo pa intravenous makonzedwe a bivarudine, ndi PT, ACT ndi APTT yayitali.Ola limodzi kapena awiri mutasiya, ACT idabwereranso pamlingo wotsogolera.