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
物理化学性质
熔点 | 129-131.5 °C(lit.) |
比旋光度 | D25 -36.5° (c = 1 in methanol) |
沸点 | 646.3±55.0 °C(Predicted) |
密度 | 1.34±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO: 5 mg/mL (11.64 mM) |
酸度系数(pKa) | pK1:4.236 (25°C) |
形态 | crystalline |
形态 | crystalline |
颜色 | light yellow |
颜色 | 淡黄色 |
CAS 数据库 | 81872-10-8(CAS DataBase Reference) |
安全数据
危险品标志 | Xn,Xi |
危险类别码 | R22-R37/38-R41 |
安全说明 | S23-S24/25 |
WGK Germany | 3 |
RTECS号 | QJ0875000 |
危险等级 | IRRITANT |
常见问题列表
佐芬普利为首个含有巯基的长效ACE抑制剂,由于其含有巯基,因此使之具有亲脂性和抗氧化特性,本品可水解为活性物佐芬普利拉。
佐芬普利常见不良反应为有头晕(3.9%)、疲劳(2.6%)、头痛(2.4%)、咳嗽(1.2%)、恶心或呕吐(1.2%)。
不常见的不良瓜为潮红(0.8%)、肌痉挛(0.8%)和虚弱(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.