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Substituted piperazine compounds, application method and applications thereof

A compound, nitrogen oxide technology, applied in the field of medicine, can solve the problems of reducing the concentration of serotonin and reducing the release of serotonin

Active Publication Date: 2016-07-06
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But after using SSRIs, it also activates 5-HT in the presynaptic membrane 1A Autoreceptors, resulting in decreased release of serotonin, lowering intersynaptic serotonin concentration

Method used

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  • Substituted piperazine compounds, application method and applications thereof
  • Substituted piperazine compounds, application method and applications thereof
  • Substituted piperazine compounds, application method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 19-32

[0373] Synthesis of target compound in Table A embodiment 19-32 of the present invention

[0374]

[0375]

[0376]

[0377] biological test

Embodiment A

[0378] Example A: Compounds in rat synaptosomes on [ 3 Analysis of the inhibitory effect of H]5-HT uptake

[0379] experiment method

[0380] At 37°C, add to buffer (106.2mMNaCl, 4.5mMKCl, 2.25mMMgSO 4 ,1.08mMNaH 2 PO 4 ,22.5mM NaHCO 3 , 9.9 mM glucose, 9 μM GTA and 45 μM ascorbic acid (pH 7.4)), synaptosomes (150 μg) with 0.1 μCi[ 3 H] In the mixed system formed by 5-hydroxytryptamine, add test compound or positive drug or negative control, and incubate for 15 minutes.

[0381] Imipramine is used as a standard positive compound for inhibiting the uptake of serotonin. Add 10 μM imipramine to the same mixed system as above to block the uptake of serotonin, and incubate at 4°C for 15 minutes to measure the activity value of the basic control . Through experiments, the uptake inhibition value of different concentrations of imipramine on rat brain synaptosomes was tested, and an inhibition curve was made.

[0382] After incubation, the sample was quickly filtered t...

Embodiment B

[0388] Example B: h5-HT 1A Receptor Binding Affinity Assay

[0389] experiment method

[0390] Homogenate (36μg protein) to human HEK-293 cell membrane at 22°C, 0.3nM[ 3 H]8-OH-DPAT (Perkin-Elmer) and buffer (50mM Tris-HCl (pH7.4), 10mMMgSO 4 , 0.5mM EDTA, 2μg / mlaprotinine) into the mixed system formed, with or without adding the test compound, and incubated for 60 minutes.

[0391] The standard reference compound is 8-OH-DPAT, and 10 μM 8-OH-DPAT is added to the mixed system under the above conditions to measure the non-specific binding value. The data of series concentrations of 8-OH-DPAT were tested in different experiments to obtain the competition curve.

[0392] After incubation, the sample was quickly filtered through a glass fiber filter (GF / B, Packard) pre-soaked with 0.3% PEI using a 96-sample cell harvester (Unifilter, Packard) under vacuum, and rinsed repeatedly with ice-cold 50 mM Tris-HCl. several times. Filters were dried and residual radioactivity...

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PUM

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Abstract

The invention discloses substituted piperazine compounds, an application method and applications thereof. Specifically, the invention relates to piperazine compounds and pharmaceutical compositions thereof for inhibiting reuptake of 5-hydroxytryptamine and / or stimulation of 5-HT1A acceptor. The invention also relates to a preparation method of the compounds and pharmaceutical compositions thereof, and an application of the compounds and pharmaceutical compositions thereof in the treatment of central nervous system dysfunction.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a substituted piperazine compound, a composition and a use method and application for treating central nervous system dysfunction. In particular, what is described in the present invention can be used as a serotonin reuptake inhibitor or / and 5-HT 1A Agonists of piperazine compounds. Background technique [0002] Serotonin, a neurotransmitter that transmits signals in the brain and nervous system, plays an important role in central nervous system (CNS) dysfunction, especially anxiety, depression, aggression and impulsive mood. Antagonizing or stimulating certain types of 5-HT receptors can effectively regulate central nervous system dysfunction. To date, at least 14 serotonin receptors have been identified. These receptors can be divided into different families, respectively recorded as 5-HT 1 , 5-HT 2 , 5-HT 3 , 5-HT 4 , 5-HT 5 , 5-HT 6 and 5-HT 7 , and th...

Claims

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Application Information

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IPC IPC(8): C07D403/12C07D413/12A61K31/517A61K31/496A61P25/24A61P25/22A61P25/18A61P25/20A61P25/00A61P25/14A61P25/28A61P25/16A61P25/30A61P15/00
Inventor 张英俊金传飞谢洪朋梁海平
Owner SUNSHINE LAKE PHARM CO LTD
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