计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
充氩,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics
In Vivo
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Sigma receptor,5-HT2 receptor,D2 receptor
规格
规格或纯度
10mM in DMSO
英文名称
DuP 734
生化机理
DuP 734 是一种西格玛受体拮抗剂。DuP 734 是一种选择性强的 sigma 和 5-HT2 受体配体，对 D2 受体的亲和力较弱。DuP 734 可能具有抗精神病活性，但不会产生典型的神经抑制剂的运动副作用。
储存条件
充氩,-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CC1CN2CCC(CC2)CC(=O)C3=CC=C(C=C3)F.Br
关联CAS
PubChem CID
MeSH Entry Terms
1-(cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl)piperidine;DuP 734;DuP-734
分子量
356.27
技术文档
高级数据
关联靶点（人）
SIGMAR1
Tclin
Sigma 非阿片类细胞内受体 1(Sigma non-opioid intracellular receptor 1)
(1 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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