Ka hope

ʻO Apixaban kahi mea koho nui a hiki ke hoʻololi i ka Factor Xa me nā helu Ki o 0.08 nM a me 0.17 nM i ke kanaka a me ka rabbit, i kēlā me kēia [1].

ʻO Factor X, ʻike ʻia hoʻi e ka eponym Stuart–Prower factor, he enzyme o ka coagulation cascade.Hoʻohana ʻia ka Factor X, ma ka hydrolysis, i ka helu Xa e nā mea ʻelua IX.ʻO Factor Xa ke ʻano o ka coagulation factorthrombokinase. Hiki i ka Inhibiting Factor Xa ke hāʻawi i kahi ala ʻē aʻe no ka anticoagulation.He mau anticoagulants kaulana ka Direct Xa inhibitors [2].

In vitro: Ua hōʻike ʻo Apixabanhas i kahi kiʻekiʻe o ka potency, selectivity, a me ka pono ma ka Factor Xa me Ki o 0.08 nM a me 0.17 nM no Human Factor Xa a me Rabbit Factor Xa, kēlā me kēia [1].Ua hoʻolōʻihi ʻia ʻo Apixaban i nā manawa clotting o ka plasma kanaka maʻamau me nā manaʻo (EC2x) o 3.6, 0.37, 7.4 a me 0.4 μM, i koi ʻia e pālua i ka manawa prothrombin (PT), ka manawa prothrombin i hoʻololi ʻia (mPT), ka manawa thromboplastin ʻāpana. APTT) a me HepTest.Ma waho aʻe, ua hōʻike ʻo Apixaban i ka mana kiʻekiʻe loa i ke kanaka a me ka rabbit plasma, akā ʻoi aku ka liʻiliʻi o ka ʻiole a me ka plasma ʻīlio ma ka PT a me ka APTT assays [3].

In vivo: Ua hōʻike ʻo Apixaban i nā pharmacokinetics maikaʻi loa me ka haʻahaʻa haʻahaʻa loa (Cl: 0.02 L kg-1h-1), a me ka haʻahaʻa haʻahaʻa o ka hāʻawi ʻana (Vdss: 0.2 L/kg) i ka ʻīlio.Ma waho aʻe, ua hōʻike pū ʻo Apixaban i ka hapalua o ke ola me T1 / 2 o 5.8 mau hola a me ka bioavailability waha maikaʻi (F: 58%) [1].I loko o ka arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) a me electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban i hoʻopuka i nā hopena antithrombotic me EC50 o 270 nM, 110 nM a me 70 nM ma ke ʻano pili i ka dose [3]. ].Ua kāohi nui ʻo Apixaban i ka hana Xa me kahi IC50 o 0.22 μM i ka rabbit ex vivo [4].I loko o ka chimpanzee, ua hōʻike pū ʻo Apixaban i ka puʻupuʻu liʻiliʻi o ka hāʻawi ʻana (Vdss: 0.17 L kg-1), ka hoʻomaʻemaʻe ʻōnaehana haʻahaʻa (Cl: 0.018 L kg-1h-1), a me ka bioavailability waha maikaʻi (F: 59%) [5].

Kuhikuhi:
Pinto DJP, Orwat MJ, Koch S, a me al.ʻIke ʻia o 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), he mea hoʻopaneʻe ikaika loa, koho, efficacious, a me ka waha bioavailable o ke koko coagulation factor Xa[J].Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
ʻO Sidhu P S. Nā mea hōʻemi pololei Xa ma ke ʻano he Anticoagulants [J].
Wong PC, Crain EJ, Xin B, a me al.ʻO Apixaban, he mea hoʻopaneʻe Xa o ka waha, pololei a koho nui loa: in vitro, antithrombotic and antihemostaticstudies [J].Ka Nupepa o Thrombosis a me Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics a me pharmacodynamics o ka mea Xa inhibitor apixaban i loko o ka lapiti [J].Nūpepa o ka thrombosis a me ka thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.ʻO nā pharmacokinetics preclinical a me nā lāʻau lapaʻau o apixaban, kahi mea hoʻopaʻapaʻa ikaika a koho Xa [J].ʻO ka puke pai ʻEulopa o ka metabolism lāʻau a me nā pharmacokinetics, 2011, 36 (3): 129-139.

ʻO Apixaban kahi mea koho nui a hiki ke hoʻololi i ka Factor Xa me nā helu Ki o 0.08 nM a me 0.17 nM i ke kanaka a me ka rabbit, i kēlā me kēia [1].

ʻO Factor X, ʻike ʻia hoʻi e ka eponym Stuart–Prower factor, he enzyme o ka coagulation cascade.Hoʻohana ʻia ka Factor X, ma ka hydrolysis, i ka helu Xa e nā mea ʻelua IX.ʻO Factor Xa ke ʻano o ka coagulation factorthrombokinase. Hiki i ka Inhibiting Factor Xa ke hāʻawi i kahi ala ʻē aʻe no ka anticoagulation.He mau anticoagulants kaulana ka Direct Xa inhibitors [2].

In vitro: Ua hōʻike ʻo Apixabanhas i kahi kiʻekiʻe o ka potency, selectivity, a me ka pono ma ka Factor Xa me Ki o 0.08 nM a me 0.17 nM no Human Factor Xa a me Rabbit Factor Xa, kēlā me kēia [1].Ua hoʻolōʻihi ʻia ʻo Apixaban i nā manawa clotting o ka plasma kanaka maʻamau me nā manaʻo (EC2x) o 3.6, 0.37, 7.4 a me 0.4 μM, i koi ʻia e pālua i ka manawa prothrombin (PT), ka manawa prothrombin i hoʻololi ʻia (mPT), ka manawa thromboplastin ʻāpana. APTT) a me HepTest.Ma waho aʻe, ua hōʻike ʻo Apixaban i ka mana kiʻekiʻe loa i ke kanaka a me ka rabbit plasma, akā ʻoi aku ka liʻiliʻi o ka ʻiole a me ka plasma ʻīlio ma ka PT a me ka APTT assays [3].

In vivo: Ua hōʻike ʻo Apixaban i nā pharmacokinetics maikaʻi loa me ka haʻahaʻa haʻahaʻa loa (Cl: 0.02 L kg-1h-1), a me ka haʻahaʻa haʻahaʻa o ka hāʻawi ʻana (Vdss: 0.2 L/kg) i ka ʻīlio.Ma waho aʻe, ua hōʻike pū ʻo Apixaban i ka hapalua o ke ola me T1 / 2 o 5.8 mau hola a me ka bioavailability waha maikaʻi (F: 58%) [1].I loko o ka arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) a me electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban i hoʻopuka i nā hopena antithrombotic me EC50 o 270 nM, 110 nM a me 70 nM ma ke ʻano pili i ka dose [3]. ].Ua kāohi nui ʻo Apixaban i ka hana Xa me kahi IC50 o 0.22 μM i ka rabbit ex vivo [4].I loko o ka chimpanzee, ua hōʻike pū ʻo Apixaban i ka puʻupuʻu liʻiliʻi o ka hāʻawi ʻana (Vdss: 0.17 L kg-1), ka hoʻomaʻemaʻe ʻōnaehana haʻahaʻa (Cl: 0.018 L kg-1h-1), a me ka bioavailability waha maikaʻi (F: 59%) [5].

Kuhikuhi:
Pinto DJP, Orwat MJ, Koch S, a me al.ʻIke ʻia o 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl) phenyl) -4, 5, 6, 7-tetrahydro-1 H-pyrazolo [3, 4- c] pyridine-3-carboxamide (Apixaban, BMS-562247), he mea hoʻopaneʻe ikaika loa, koho, efficacious, a me ka waha bioavailable o ke koko coagulation factor Xa[J].Journal of medicinal chemistry, 2007, 50(22): 5339-5356.
ʻO Sidhu P S. Nā mea hōʻemi pololei Xa ma ke ʻano he Anticoagulants [J].
Wong PC, Crain EJ, Xin B, a me al.ʻO Apixaban, he mea hoʻopaneʻe Xa o ka waha, pololei a koho nui loa: in vitro, antithrombotic and antihemostaticstudies [J].Ka Nupepa o Thrombosis a me Haemostasis, 2008, 6(5): 820-829.
Zhang D, He K, Raghavan N, et al.Metabolism, pharmacokinetics a me pharmacodynamics o ka mea Xa inhibitor apixaban i loko o ka lapiti [J].Nūpepa o ka thrombosis a me ka thrombolysis, 2010, 29 (1): 70-80.
He K, Luettgen JM, Zhang D, et al.ʻO nā pharmacokinetics preclinical a me nā lāʻau lapaʻau o apixaban, kahi mea hoʻopaʻapaʻa ikaika a koho Xa [J].ʻO ka puke pai ʻEulopa o ka metabolism lāʻau a me nā pharmacokinetics, 2011, 36 (3): 129-139.

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