布那司特
中文名称 | 布那司特 |
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中文同义词 | 布那司特;化合物 T17191;BUNAPROLAST (U66858) |
英文名称 | 1-Acetoxy-2-butyl-4-methoxynaphtalene |
英文同义词 | 1-Acetoxy-2-butyl-4-methoxynaphtalene;Bunaprolast;1-Acetoxy-2-butyl-4-methoxynaphthalene;U-66858;1-acetoxy-2-n-butyl-4-methoxynaphthalene;1-Naphthalenol, 2-butyl-4-methoxy-, 1-acetate;Bunaprolast (U66858) |
CAS号 | 99107-52-5 |
分子式 | C17H20O3 |
分子量 | 272.3389 |
EINECS号 | |
相关类别 | |
Mol文件 | 99107-52-5.mol |
结构式 |
布那司特 性质
储存条件 | Store at -20°C |
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溶解度 | 溶于二甲基亚砜 |
LTB 4
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TXB 2
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5-LO
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Bunaprolast (U-66,858) undergoes deacetylation to an initial metabolite with similar pharmacological potency. The inhibitory effects of the semi-quinone Bunaprolast and its metabolite U-68,244 on the ionophore-induced formation of leukotriene B4 (LTB4) are examined in human whole blood (WB). Preincubation of Bunaprolast and U-68,244 for 1 min prior to challenge of blood with calcium ionophore A23187 results in IC 50 s of 1080±644 and 820±442 nM, respectively. After 60 min preincubation, IC 50 s are 250±85 and 270±79 nM. The activity of the lipoxygenase inhibitor AA-861 in this system is similar to that of Bunaprolast, while vitamin K and the sulphate conjugate of Bunaprolast show significant inhibition of LTB4 release only at micromolar concentrations. Bunaprolast exhibits significant inhibition of thromboxane A2 release (p<0.02) in a comparative study with the known cyclooxygenase (CO) inhibitor Flurbiprofen.
The IgE-mediated hypersensitivity to Ascaris antigen in reactor rhesus primates is used to assess the pharmacologic profile of Bunaprolast (U-66,858). When Bunaprolast is given by the oral route, it shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes. When Bunaprolast is given by the aerosol route, it shows dose independent inhibition. In 15 animals, aerosols (52±32 to 53±10% for RL, p=0.05 and 45±19 to 28±19% Cdyn inhibitions, p=0.05) for 5.0-0.1% aerosol. By the oral route, inhibition is seen at 1-4 h following administration. In 5 animals, oral doses of 10 and 5 mg/kg inhibit (RL by 98±2 to 78±1.5%, p=0.01 and Cdyn by 75±17 to 60.9±9.1%, p=0.05) by 10 and 5 mg/kg Bunaprolast, respectively.