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

Boc-Arg (Pbf) -OH shine tushen arginine.
Bivalirudine, maganin maganin jijiyoyi na roba wanda dan uwan ​​20-peptide ne na hirudin, an amince da shi don siyarwa a Amurka a shekara ta 2000. Allurar farar fata ce, sako-sako da sinadarai ko amorphous m.Bivarudine na iya ɗaure musamman ga thrombin catalytic site da kuma anion waje dauri site, da kuma kai tsaye hana ayyukan thrombin, don haka hana dauki catalyzed da kuma jawo ta thrombin, da kuma sakamako ne reversible.Ana amfani da Bivarudine galibi azaman maganin ɗigon jini don zaɓin shiga tsakani na jijiyoyin jini (PCI) a cikin manya.
Bivarudine shine mai hana thrombin kai tsaye, wanda ke ɗaure musamman ga wuraren catalytic da wuraren dauri na anion na thrombin kyauta kuma akan thrombus.Tsarin ɗaure tsakanin bivaludine da thrombin yana canzawa, kuma thrombin zai iya dawo da ainihin aikin ilimin halitta na thrombin ta hanyar enzymolysis na sannu a hankali na haɗin peptide tsakanin bivaludine Arg3-Pro4.
Nazarin a cikin vitro ya nuna cewa bivarudine ba zai iya hana thrombin kyauta ba kawai, amma kuma yana hana thrombin daure tare da ɗigon jini ba tare da an cire shi daga abubuwan da aka saki ta platelets ba.Yana iya tsawaita lokacin prothrombin na ɓangare (APTT), lokacin thrombin (TT), lokacin prothrombin (PT) da lokacin coagulation mai aiki (ACT) wanda plasma na al'ada ke kunna.Akwai dangantaka ta layi tare da maida hankali na bivarudine, amma ko wannan alaƙar ta wanzu a aikace-aikacen asibiti ba a sani ba.
An ba da rahoto a cikin wallafe-wallafen cewa magungunan magunguna na marasa lafiya da ke fama da cututtukan zuciya na zuciya (PTCA) sun kasance masu layi bayan gudanarwar bivarudine na cikin jini.An ba mai haƙuri 1 mg / kg a cikin jini a matsayin nauyin nauyin nauyi, sannan kuma wani jiko na IV na 2.5 mg / kg / hr don 4 hours, wanda ya daidaita a 12.3 ± 1.7 mg / ml a cikin vivo.An cire Bivarudine daga plasma ta hanyar hydrolysis na koda da lalata protease.Rabin rabin rayuwar marasa lafiya tare da aikin koda na al'ada shine kusan 25min, kuma an tsawaita rabin rayuwar marasa lafiya tare da matsakaicin matsakaici da ƙarancin ƙarancin koda.Kimanin kashi 25% na bivarudine ana iya cire su ta hanyar dialysis kuma a share su ta hanyar hemodialysis.Ya kamata a kula da ACT a cikin marasa lafiya da nakasa na koda.A cikin masu aikin sa kai masu lafiya, an lura da tasirin anticoagulant nan da nan bayan gudanar da bivarudine na cikin jijiya, tare da tsawan lokaci PT, ACT da APTT.Sa'o'i daya zuwa biyu bayan janyewar, ACT ta koma matakin gudanarwa na farko.