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

Boc-Arg (Pbf) -OH ni inkomoko ya arginine.
Bivalirudine, anticagulant ya sintetike ni mubyara wa peptide 20 wa hirudin, yemerewe kugurishwa muri Amerika mu 2000. Gutera inshinge ni ibintu byera, birekuye cyangwa bikomeye bya amorphous.Bivarudine irashobora guhuza byumwihariko kurubuga rwa catalitiki ya trombine hamwe na anion yo hanze ihuza, kandi ikabuza byimazeyo ibikorwa bya trombine, bityo bikabuza reaction yatangijwe kandi iterwa na trombine, kandi ingaruka zayo zirahinduka.Bivarudine ikoreshwa cyane nka anticoagulant kugirango itoranyirize hamwe (PCI) kubantu bakuru.
Bivarudine ni inhibitori ya trombine itaziguye, ihuza cyane na site ya catalitiki hamwe na anion exo-binding site ya trombine yubusa no kuri trombus.Inzira yo guhuza hagati ya bivaludine na trombine irahindurwa, kandi trombine irashobora kugarura ibikorwa byambere byibinyabuzima bya trombine hakoreshejwe enzymolysis gahoro gahoro ya peptide hagati ya bivaludine Arg3-Pro4.
Mu bushakashatsi bwa vitro bwerekanye ko bivarudine idashobora gusa kubuza trombine yubusa gusa, ahubwo inabuza trombine guhambira hamwe nudutsi tutabangamiwe nibintu byasohowe na platine.Irashobora kongera igihe cya prothrombin igice (APTT), umwanya wa trombine (TT), igihe cya prothrombine (PT) nigihe cyo gukora coagulation (ACT) gikoreshwa na plasma isanzwe.Hariho umurongo umwe hamwe na concentration ya bivarudine, ariko niba iri sano rihari mugukoresha amavuriro ntibisobanutse.
Mu bitabo byavuzwe ko pharmacokinetics y’abarwayi batewe na coronary angioplasty (PTCA) itandukanijwe nyuma yubuyobozi bwimitsi ya bivarudine.Umurwayi yahawe mg / kg 1 mu mitsi nk'umuzigo uremereye, hanyuma akurikirwa n'indi IV ya mg / kg / hr mu masaha 4, ihagarara kuri 12.3 ± 1.7 mg / ml muri vivo.Bivarudine ikurwa muri plasma na hydrolysis yimpyiko no kwangirika kwa protease.Igice cya kabiri cyubuzima bwabarwayi bafite imikorere isanzwe yimpyiko ni nka 25min, kandi igice cya kabiri cyubuzima bwabarwayi bafite ikibazo cyo kubura impyiko zidakabije kandi zikomeye kongerewe.Hafi ya 25% ya bivarudine irashobora gukurwaho na dialyse hanyuma igahanagurwa na hemodialyse.ACT igomba gukurikiranwa kubarwayi bafite ubumuga bwimpyiko.Mu bakorerabushake bafite ubuzima bwiza, ingaruka za anticoagulant zahise zigaragara nyuma yubuyobozi bwimitsi ya bivarudine, hamwe na PT, ACT na APTT igihe kirekire.Nyuma yisaha imwe cyangwa ibiri nyuma yo gukuramo, ACT yagarutse kurwego rwubuyobozi.