- Synthesis and biological evaluation of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors
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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.
- Lapa, Gennady B.,Lapa, Alla A.
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p. 203 - 205
(2019/04/25)
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- NPY ANTAGONISTS, PREPARATION AND USES
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The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
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Page/Page column 57-58
(2009/09/28)
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- The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines
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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.
- Lapa, Gennady B.,Byrd, Gary D.,Lapa, Alla A.,Budygin, Evgeny A.,Childers, Steven R.,Jones, Sara R.,Harp, Jill J.
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p. 4915 - 4918
(2007/10/03)
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- ENZYMATIC "IN VITRO" REDUCTIONS OF KETONES. PART 12. REDUCTION OF 1-ALKYL-4-PIPERIDONES IN AN ETHANOL-NAD+-HLAD-SYSTEM.
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The steady state initial rate equation for a ketone-ethanol-NAD+-HLAD recycling system is checked for 1-n-butyl-4-piperidone.All reaction parameters are discussed in order to optimize the reduction of this substrate.For a series of 1-alkyl-4-piperidones the thermodynamic activation parameters for the reduction in this system are determined and discussed.
- Luppen, Jaymes Van,Lepoivre, Jozef,Lemiere, Guy,Alderweireldt, Frank
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p. 749 - 761
(2007/10/02)
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