DUP 734
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- CAS号:
- 135135-87-4
- 英文名:
- DuP 734
- 英文别名:
- DuP 734;2-[1-(cyclopropylmethyl)piperidin-4-yl]-1-(4-fluorophenyl)ethanone;2-[1-(Cyclopropylmethyl)Piperidin-4-Yl]-1-(4-Fluorophenyl)Ethanone Hydrobromide
- 中文名:
- DUP 734
- 中文别名:
- CBNumber:
- CB51397821
- 分子式:
- C17H22FNO.BrH
- 分子量:
- 356.277
- MOL File:
- 135135-87-4.mol
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DUP 734化学性质
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储存条件:
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4°C, stored under nitrogen, away from moisture
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溶解度:
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DMSO : 250 mg/mL (701.71 mM)
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形态:
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Solid
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颜色:
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Off-white to light yellow
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DUP 734性质、用途与生产工艺
DuP 734 是一种 sigma 受体拮抗剂,DuP 734 是一种有效的选择性 sigma 和 5-HT2 受体配体,对 D2 受体的亲和力弱。DuP 734 具有抗精神病活性,而没有抗精神病剂常见的副作用。
Sigma receptor; 5-HT2 receptor; D2 receptor
DuP 734 potently blocks mescaline-induced scratching (ED
50
=0.35 mg/kg, p.o.) and aggressive activity (ED
50
=1.9 mg/kg, p.o.) and is relatively much weaker as an apomorphine antagonist (ED
50
=12 mg/kg, p.o.).
Administration of DuP 734 potently antagonizes the binding of [
3
H]DuP 734 and [
3
H](+)-SKF 10,047 to brain sigma receptors in vivo with ID
50
values of 0.02 and 0.07 mg/kg (0.07 and 0.25μmol/kg), respectively.
Following intravenous dosing, the disposition of DuP 734 in mice, rats, beagle dogs and cynomolgus monkeys is characterized by high total body systemic plasma clearance (46 to 87 mL/min/kg) and large steady-state volume of distribution (3.6 to 6.8 L/kg). The terminal elimination half-life ranged from 50 to 83 min. The gastrointestinal absorption from an aqueous solution is very rapid in mice and rats with peak DuP 734 plasma concentrations attain within 5 and 20 min following administration, respectively. The peak plasma concentrations in dogs and monkeys are attained within 45 and 130 min, respectively. The absolute bioavailability in mice ranges from 29 to 46% at doses of 3.1 to 30.1 mg/kg. The bioavailability increases from 4 to 10% and from 14 to 72% when doses are increased from 12.5 to 50 mg/kg and 1 to 3 mg/kg of DuP 734 in rats and dogs, respectively. The bioavailability in monkeys is 30.5% at 9.3 mg/kg DuP 734 dose. The dose dependent pharmacokinetics of DuP 734 is observed within narrow dose ranges in all animal species investigated.
DUP 734
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-136281 | DuP 734 | 135135-87-4 | 5mg | 2500元 |
2024/04/30 | HY-136281 | DuP 734 | 135135-87-4 | 10mM * 1mLin DMSO | 2750元 |
135135-87-4, DUP 734 相关搜索:
- C17H23BrFNO
- 135135-87-4
- 2-[1-(Cyclopropylmethyl)Piperidin-4-Yl]-1-(4-Fluorophenyl)Ethanone Hydrobromide
- 2-[1-(cyclopropylmethyl)piperidin-4-yl]-1-(4-fluorophenyl)ethanone
- DuP 734