91600-10-1Relevant academic research and scientific papers
Short-acting biquaternary ammonium compound as well as preparation method and application thereof
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Paragraph 0070-0073, (2021/06/02)
The invention provides a short-acting biquaternary ammonium compound as well as a preparation method and application thereof. The biquaternary ammonium compound is represented by a formula (I). The compound disclosed by the invention has quick-acting and ultra-short-acting non-depolarized muscle relaxation molecular activity, is quick in acting and can generate a complete muscle relaxation effect under the condition of low administration dosage, and the time required for complete recovery of muscle strength is short and is obviously shorter than that of a positive drug cisatracurium and a depolarized muscle relaxation drug succinylcholine; the problems of non-depolarized muscle relaxant in the prior art are effectively solved, and the compound can be used for preparing the non-depolarized muscle relaxant with an excellent effect and has a good prospect.
Synthesis and biological evaluation of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors
Lapa, Gennady B.,Lapa, Alla A.
, p. 203 - 205 (2019/04/25)
The library of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors was designed and synthesized. H-Bond donors in piperidine ring were found to be important for reduced locomotor activity in mice. 4-[Bis(4-fluorophenyl)methoxy]piperidine has IC50 17.0 ± 1.0 nm for dopamine transporter and locomotor activity, which is lower than that for cocaine.
The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines
Lapa, Gennady B.,Byrd, Gary D.,Lapa, Alla A.,Budygin, Evgeny A.,Childers, Steven R.,Jones, Sara R.,Harp, Jill J.
, p. 4915 - 4918 (2007/10/03)
The synthesis of potent 4-aryl methoxypiperidinol inhibitors of the dopamine transporter is described. Symmetrical para substituents of the benzene rings are important for high potency in binding to the dopamine transporter. 4-[Bis(4-fluorophenyl) methoxy]-1-methylpiperidine has an IC50 of 22.1 ± 5.73 nM and increases locomotor activity in mice.
