货号 | 16214-1g |
描述 | Benztropine is a synthetic compound derived from the combination of atropine and diphenhydramine that acts centrally to antagonize M1 muscarinic acetylcholine receptors (Ki = 0.59 nM in rat).1 It can also increase the availability of dopamine by inhibiting uptake through the dopamine transporter (Ki = 160 nM).2,3 Benztropine has been used in the management of Parkinson’s disease symptoms to address involuntary tremor and dystonia.4 It has also been identified as a functional inhibitor of acid sphingomyelinase.5 |
别名 | Cogentin®;NSC 169913; |
供应商 | Cayman |
应用文献 | |
1.Zhang, Y.,Joseph, D.B.,Bowen, W.D., et al. Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues. J.Med.Chem 44(23), 3937-3945 (2001). 2.Schmitt, K.C.,Zhen, J.,Kharkar, P., et al. Interaction of cocaine-, benztropine-, and GBR12909- like compounds with wildtype and mutant human dopamine transporters: Molecular features that differentially determine antagonist binding properties. Journal of Neurochemistry 107(4), 928-940 (2008). 3.Ukairo, O.T.,Bondi, C.D.,Newman, A.H., et al. Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue. Journal of Pharmacology and Experimental Therapeutics 314(2), 575-583 (2005). 4.Brocks, D.R. Anticholinergic drugs used in Parkinson’s disease: An overlooked class of drugs from a pharmacokinetic perspective. Journal of Pharmacy & Pharmaceutical Sciences 2(2), 39-46 (1999). 5.Kornhuber, J.,Muehlbacher, M.,Trapp, S., et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One 6(8), 1-13 (2011). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 403.5 |
分子式 | C21H25NO • CH3SO3H |
CAS号 | 132-17-2 |
稳定性 | ≥ 2 years |
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