Benztropine mesylate
(Synonyms: 甲磺酸苯扎托品; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate) 目录号 : GC16791An M1 muscarinic acetylcholine receptor antagonist
Cas No.:132-17-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Benzatropine mesylate is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease.Target: mAChRBenzatropine mesylate is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics. Symptoms of Parkinson's disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzatropine mesylate also produces antagonistic effects at the histamine H1 receptor [1, 2].Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). BZT analogues also exhibit varied binding affinities for muscarinic M(1) and histamine H(1) receptors. The BZT analogues showed a wide range of histamine H(1) receptor (K(i)=16-37,600 nM) and DAT (K(i)=8.5-6370 nM) binding affinities [3].
References:
[1]. Wszola, B.A., K.M. Newell, and R.L. Sprague, Risk factors for tardive dyskinesia in a large population of youths and adults. Exp Clin Psychopharmacol, 2001. 9(3): p. 285-96.
[2]. van Harten, P.N., et al., Intermittent neuroleptic treatment and risk for tardive dyskinesia: Curacao Extrapyramidal Syndromes Study III. Am J Psychiatry, 1998. 155(4): p. 565-7.
[3]. Kulkarni, S.S., et al., Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem, 2006. 14(11): p. 3625-34.
Cas No. | 132-17-2 | SDF | |
别名 | 甲磺酸苯扎托品; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate | ||
化学名 | 3-benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane;methanesulfonic acid | ||
Canonical SMILES | CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4.CS(=O)(=O)O | ||
分子式 | C21H25NO.CH4SO3 | 分子量 | 403.53 |
溶解度 | ≥ 20.18mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4781 mL | 12.3907 mL | 24.7813 mL |
5 mM | 0.4956 mL | 2.4781 mL | 4.9563 mL |
10 mM | 0.2478 mL | 1.2391 mL | 2.4781 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。