您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > L-DOPA methyl ester(hydrochloride)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
L-DOPA methyl ester(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-DOPA methyl ester(hydrochloride)图片
CAS NO:1421-65-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
500mg电议
1g电议
5g电议

产品介绍
Cas No.1421-65-4
别名盐酸左旋多巴甲酯,3,4-Dihydroxyphenylalanine methyl ester,LDME,Levodopa methyl ester,ST 41769
化学名3-hydroxy-L-tyrosine, methyl ester, monohydrochloride
Canonical SMILESOC1=C(O)C=CC(C[C@H](N)C(OC)=O)=C1.Cl
分子式C10H13NO4o HCl
分子量247.7
溶解度≥ 13.6mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

L-DOPA methyl ester is a dopamine D1 receptor agonist.

The D1 subtype of the dopamine receptor is the most abundant dopamine receptor in the central nervous system. D1 receptors can regulate neuronal growth and development, mediate some behavioral responses, and modulate dopamine receptor D2-mediated events.

In vitro: L-DOPA methyl ester is a neutral derivative of L-DOPA formulated for increased solubility compared to the parent compound. L-DOPA is a metabolic precursor of dopamine that is capable of crossing the blood brain barrier to act as a dopamine D1 receptor agonist [1].

In vivo: On intraperitoneal or subcutaneous administration to mice L-Dopa methyl ester was found to be equivalent to L-Dopa in reversing reserpine-induced akinesia and producing contraversive circling behaviour in rats. On oral administration the methyl ester was even more active. The administration of L-Dopa or the methyl ester had equivalent changes of metabolite levels in striatal and mesolimbic dopamine, homovanillic acid, as well as 3,4-dihydroxyphenylacetic acid [2].

Clinical trial: Five sublingual and five subcutaneous doses of L-dopa methyl ester were given to seven patients with idiopathic Parkinson's disease and motor fluctuations. Motor assessments were conducted using the modified Webster scale. Results showed that two patients switched "on" with subcutaneous L-dopa methyl ester with the same quality and duration of therapeutic effect seen after their oral levodopa doses. The time from injection to full switch "on" was 60 minutes in both patients. Two patients had no effect over the entire observation period of 90 minutes and another one experienced onset-of-dose dyskinesias continuing for 110 minutes without ever switching fully "on" [3].

References:
[1] Berends, H. I.,Nijlant, J.M.M.,Movig, K.L.L., et al. The clinical use of drugs influencing neurotransmitters in the brain to promote motor recovery after stroke; a Cochrane systematic review. European Journal of Physical and Rehabilitation Medicine 45(4), 621-630 (2009).
[2] Cooper DR, Marrel C, Testa B, van de Waterbeemd H, Quinn N, Jenner P, Marsden CD.  L-Dopa methyl ester--a candidate for chronic systemic delivery of L-Dopa in Parkinson's disease. Clin Neuropharmacol. 1984;7(1):89-98.
[3] Kleedorfer, B. ,Lees, A.J. and Stern, G.M. Subcutaneous and sublingual levodopa methyl ester in Parkinson’s disease. J.Neurol.Neurosurg.Psychiatry 54(4), 373 (1991).