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CAS: 27833-64-3
分子式: C7H10NNaaO7P2
分子量: 445.90
中文名称: 
丁二酸洛沙平
英文名称: 
succinic acid, compd. with 2-chloro-11-(4-methyl-1-piperazinyl)dibenz(b,f)(1,4)
oxazepine (1:1)
cl 71563
daxoline
lederle
loxapac
loxapine succinate
loxitane
succinic acid, compd. with2-chloro-11-(4-methyl-1-piperazinyl)dibenz(b,f)(1,4) oxazepine (1:1)
Loxapine Succinate Capsules
用途: 治疗精神分裂症丁二酸洛沙平是二苯并氧氮杂卓的三环化合物。动物试验证明,丁二酸洛沙平能对抗由阿朴吗啡致大鼠的定向行为;能阻断由阿朴吗啡致小鼠的攀爬行为;与戊巴比妥钠有协同作用;能不同程度地阻断小鼠的打斗行为,并对中枢兴奋剂苯丙胺致小鼠死亡有一定的保护作用。上述作用与抗精神病作用有关,目前认为丁二酸洛沙平的抗精神病作用机理主要是阻断中枢多巴胺受体,有镇静和对攻击行为的抑制作用,尤其对兴奋、攻击性行为的精神分裂症有效。
推荐供应商
货号品牌产品名称规格包装、参考价格详情
L794688MACKLIN丁二酸洛沙平10mM in DMSO514元/1ml;  
储存:-20°C
L831270MACKLIN丁二酸洛沙平99%374元/50mg;  
储存:室温,密封
状态:白色粉末
303244J&KLidocaine succinate98%, 一种5羟-色胺受体抑制剂, 多巴胺受体670元/250MG;   1541元/1G;   2300元/5G;  

基本信息

分子式C22H24ClN3O5
分子量445.90
熔点150-152
沸点458.6
闪点231.1
MDL编码MFCD00069298
EINECS 编号248-682-0
存储条件Freezer -20℃

产品描述

Loxapine Succinate是D2DR和D4DR抑制剂,5-羟色胺受体拮抗剂,也是Dibenzoxazepine类的抗精神病试剂。

靶点(IC50 & Targe)

5-HT2 (bovine),6.8nM(Ki)

5-HT2 (human),6.2nM(Ki)

D2,24nM(Ki)

D4,7.5nM(Ki)

体外研究

Loxapine存在时, [3H]Ketanserin 结合到人和牛大脑额叶皮层上的5-HT2受体,Ki分别为6.2 nM 和 6.6 nM。 在涉及人体细胞膜比较竞争实验中,Loxapine各种有效受体的排名顺序如下:5-HT2≥D4>>>D1>D2。[1] 0.2 μM, 2 μM 和 20 μM Loxapine处理脂多糖激活的胶质细胞混合培养,1和3天后,降低IL-1beta分泌。0.2 μM, 2 μM 和 20 μM Loxapine处理胶质细胞混合培养,1和3天后,降低IL-2分泌。此外,2 μM, 10 μM 和 20 μM Loxapine处理LPS诱导的小胶质细胞混合培养,降低IL-1beta分泌。[2]

体内研究

Loxapine(5 mg/kg) 每天注射给药大鼠,4周或10周后,显著降低Serotonin (S2)受体密度(超过 50%) 。Loxapine (5 mg/kg) 给药大鼠脑部,不会改变Dopamine 受体密度,但大大降低Serotonin 受体密度,达47%。[3] Loxapine 按0.3 mg/kg剂量皮下注射大鼠,引起明显的全身僵硬,45秒到5小时达到最高水平。Clozapine (10 mg/kg 皮下注射)可治疗Loxapine诱发的全身僵硬,高度僵硬状态降低到与空白对照组没有明显不同。[4]

参考文献

[1] Singh AN, et al. J Psychiatry Neurosci, 1996, 21(1), 29-35.

[2] Labuzek K, et al. Eur Neuropsychopharmacol, 2005, 15(1), 23-30.

[3] Lee T, et al. Psychiatry Res, 1984, 12(4), 277-285.

[4] Kalkman HO, et al. Naunyn Schmiedebergs Arch Pharmacol,

安全信息

WGK3
RTECSWM5750000
C46269Alfa AesarLoxapine succinate8381元/1g;  

基本信息

Ref#
46269

分子式
C18H18ClN3O.C4H6O4

分子量
406.47

L106Sigma-AldrichLoxapine succinate saltsolid698.55元/100 MG;  

产品说明

生化/生理作用

D2/D4 dopamine receptor antagonist; 5-HT2A/2B, 5-H7 serotonin receptor antagonist; dibenzoxazepine antipsychotic agent.

特点和优势

This compound was developed by Watson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

基本信息

经验(实验)分子式C18H18ClN3O · C4H6O4
分子量445.90
EC 号248-682-0
MDL编号MFCD00069298
PubChem化学物质编号24277719
NACRESNA.77

产品性质

质量水平100
形式solid
颜色 white
溶解性H2O: soluble
创始人Watson
SMILES stringCN(CC1)CCN1C2=NC3=C(C=CC=C3)OC4=C2C=C(Cl)C=C4.OC(CCC(O)=O)=O
InChI1S/C18H18ClN3O.C4H6O4/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18;5-3(6)1-2-4(7)8/h2-7,12H,8-11H2,1H3;1-2H2,(H,5,6)(H,7,8)
InChI keyYQZBAXDVDZTKEQ-UHFFFAOYSA-N
Gene Informationhuman ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
个人防护装备Eyeshields, Gloves, type N95 (US)
1370702USPLoxapine succinateUnited States Pharmacopeia (USP) Reference Standard2633.96元/125 MG;  

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.
For further information and support please go to the website of the issuing Pharmacopoeia.

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

USP issued SDS can be found here.
Sales restrictions may apply.

基本信息

经验(实验)分子式C18H18ClN3O · C4H6O4
分子量445.90
MDL编号MFCD00069298
PubChem化学物质编号329750266

产品性质

等级pharmaceutical primary standard
manufacturer/tradenameUSP
application(s)pharmaceutical (small molecule)
格式neat
SMILES stringCN(CC1)CCN1C2=NC3=C(C=CC=C3)OC4=C2C=C(Cl)C=C4.OC(CCC(O)=O)=O
InChI1S/C18H18ClN3O.C4H6O4/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18;5-3(6)1-2-4(7)8/h2-7,12H,8-11H2,1H3;1-2H2,(H,5,6)(H,7,8)
InChI keyYQZBAXDVDZTKEQ-UHFFFAOYSA-N
Gene Informationhuman ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2C(3358)

安全信息

储存分类代码6.1B - Non-combustible, acute toxic Cat. 1 and 2 / very toxic hazardous materials
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
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