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Benztropine mesylate

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Chemical Structure| 132-17-2 同义名 : 苯托品甲磺酸盐 ;Benztropine methanesulfonate;Benzotropine mesylate;ST50997629;NSC42199;MLS000737056;Cogentin;NSC 169913;Benztropine (mesylate);Cogentin mesylate;Benzatropine mesylate
CAS号 : 132-17-2
货号 : A308385
分子式 : C22H29NO4S
纯度 : 98%
分子量 : 403.535
MDL号 : MFCD00074784
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(260.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(247.81 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 60 mg/mL clear

生物活性
靶点

  • DAT

    DAT, IC50:118 nM
描述 Benztropine mesylate is a centrally acting anticholinergic agent for the treatment of Parkinson's disease. In a multiple sclerosis mouse model, benztropine mesylate induced the differentiation of oligodendrocytes through M1 and M3 muscarinic receptors and enhanced re-myelination. Benztropine mesylate also acts as an anti-histamine and a dopamine re-uptake inhibitor, and as an allosteric antagonist of the human D2 dopamine receptor. For 4T1-luc2 spheres, the IC50 value of benztropine mesylate was around 5 μM[3]. Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). The BZT analogues showed a wide range of histamine H(1) receptor (Ki=16-37,600 nM) and DAT (Ki=8.5-6370 nM) binding affinities[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01833897 Bipolar Disorder Phase 4 Completed - United States, New York ... 展开 >> New York State Psychiatric Institute New York, New York, United States, 10032 收起 <<
NCT00009672 Radiculopathy ... 展开 >> Sciatica 收起 << Phase 2 Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00167856 Neuropathic Pain ... 展开 >> Pain Spinal Cord Injuries 收起 << Not Applicable Completed - United States, Florida ... 展开 >> VA Medical Center, Miami Miami, Florida, United States, 33125 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.48mL

0.50mL

0.25mL

12.39mL

2.48mL

1.24mL

24.78mL

4.96mL

2.48mL
参考文献

[1]Simoni D, Rossi M, et al. Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter. J Med Chem. 2005 May 5;48(9):3337-43.

[2]Reith ME, Berfield JL, et al. The uptake inhibitors cocaine and benztropine differentially alter the conformation of the human dopamine transporter. J Biol Chem. 2001 Aug 3;276(31):29012-8.

[3]Cui J, Hollmén M, Li L, Chen Y, Proulx ST, Reker D, Schneider G, Detmar M. New use of an old drug: inhibition of breast cancer stem cells by benztropine mesylate. Oncotarget. 2017 Jan 3;8(1):1007-1022. doi: 10.18632/oncotarget.13537. PMID: 27894093; PMCID: PMC5352030.

[4]Kulkarni SS, Kopajtic TA, Katz JL, Newman AH. Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem. 2006 Jun 1;14(11):3625-34. doi: 10.1016/j.bmc.2006.01.017. Epub 2006 Feb 3. PMID: 16460947; PMCID: PMC1555624.