81872-10-8
基本信息
1-NAPHTHYLACETIC ACID
AKOS AU36-M588
ALPHA-NAA
ALPHA-NAPHTHALENACETIC ACID
ALPHA-NAPHTHALENEACETIC ACID
ALPHA-NAPHTHYLACETIC ACID
a-Naphthylacetic acid
FRUIT FAX(R)
NAA
NAA(R)
NAA(TM)
NAPHTHALENE-1-ACETIC ACID
NAPHTHALENEACETIC ACID
PLANOFIX
RARECHEM AL BO 0198
ROOTONE(R)
1-NAPHTHYLACETICACIDα-NAPHTHYLACETICACID
1-[(S)-3-(Benzoylthio)-2-methyl-1-oxopropyl]-4α-(phenylthio)-L-proline
S-Benzoyl-4-phenylthiocaptopril
物理化學性質(zhì)
常見問題列表
佐芬普利為首個含有巰基的長效ACE抑制劑,由于其含有巰基,因此使之具有親脂性和抗氧化特性,本品可水解為活性物佐芬普利拉。
佐芬普利常見不良反應(yīng)為有頭暈(3.9%)、疲勞(2.6%)、頭痛(2.4%)、咳嗽(1.2%)、惡心或嘔吐(1.2%)。
不常見的不良瓜為潮紅(0.8%)、肌痙攣(0.8%)和虛弱(0.5%)。
IC50: 81 μM (ACE)
Kinetic analyses demonstrate that enalapril inhibits the uptake of GlySar in a competitive manner (K i approximately 6 mM). Fosinopril and Zofenopril have the greatest inhibitory potency (IC 50 values of 55 and 81μM, respectively) while the other ACE inhibitors exhibit low-affinity interactions with the renal peptide transporter.
Zofenopril, a sulphydrylic compound, at doses higher than 70 mg/kg i.p. produces significant protection (i.e. at 70 mg/kg, P=0.044, F=2.17, d.f.=18; at higher concentration P<0.05) against the tonic phase of the audiogenic seizure response. Pretreatment with Zofenopril (15 mg/kg, i.p.) is able to produce a consistent shift to the left of the dose-response curves and a significant reduction of ED 50 values against clonus of some AEDs with the exceptions of diazepam, felbamate, phenobarbital and phenytoin compare with concurrent groups, suggesting an increase in anticonvulsant activity.