1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Selegiline

Selegiline  (Synonyms: 司来吉兰; Deprenyl; (-)-Selegiline; (-)-Deprenyl)

目录号: HY-14198
产品使用指南 技术支持

Selegiline (Deprenyl) 是一种有效、选择性和不可逆的 MAO-B 抑制剂,IC50 值为 51 nM。Selegiline 对 MAO-B 的选择性比 MAO-A 高 450 倍 (IC50=23 μM)。Selegiline 可用于帕金森氏病、阿尔茨海默病和重度抑郁症的研究。

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Selegiline Chemical Structure

Selegiline Chemical Structure

CAS No. : 14611-51-9

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  • 生物活性

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生物活性

Selegiline (Deprenyl) is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). Selegiline can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive disorder[1][2][3].

IC50 & Target[1]

MAO-B

51 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BTI-TN-5B1-4 IC50
0.017 μM
Compound: Deprenyl
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay
[PMID: 22005185]
BTI-TN-5B1-4 IC50
0.019 μM
Compound: Selegiline
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method
[PMID: 22222137]
BTI-TN-5B1-4 IC50
0.019 μM
Compound: (R)(-)D
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay
[PMID: 20045650]
BTI-TN-5B1-4 IC50
0.0196 μM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay
[PMID: 23927971]
BTI-TN-5B1-4 IC50
0.02 μM
Compound: R-(-)-deprenyl
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
[PMID: 20715818]
BTI-TN-5B1-4 IC50
0.02 μM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
[PMID: 23474901]
BTI-TN-5B1-4 IC50
0.02 μM
Compound: (R)-(-)-deprenyl
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method
[PMID: 19267475]
BTI-TN-5B1-4 IC50
0.0386 μM
Compound: (R)-(-)-Deprenyl
Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
[PMID: 31711793]
BTI-TN-5B1-4 IC50
14.8 nM
Compound: R-(-)-Deprenyl
Inhibition of human recombinant MAO-B expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method
Inhibition of human recombinant MAO-B expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method
[PMID: 21316817]
BTI-TN-5B1-4 IC50
1424 nM
Compound: Selegiline
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
[PMID: 31265934]
BTI-TN-5B1-4 IC50
1424 nM
Compound: Selegiline
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
[PMID: 30522087]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: D
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
[PMID: 23153812]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: D
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
10.1039/C0MD00014K
BTI-TN-5B1-4 IC50
19.6 nM
Compound: Selegiline
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method
[PMID: 21405131]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: (R)-(-)-Deprenyl
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
[PMID: 24746464]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: R(-)deprenyl
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
[PMID: 21872365]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: Selegiline
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production
Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production
[PMID: 25532905]
BTI-TN-5B1-4 IC50
19.6 nM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
[PMID: 27135371]
BTI-TN-5B1-4 IC50
20 nM
Compound: R-(-)-deprenyl
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
[PMID: 20579890]
BTI-TN-5B1-4 IC50
20.1 μM
Compound: (R)-(-)-Deprenyl
Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
[PMID: 31711793]
BTI-TN-5B1-4 IC50
5.5 nM
Compound: Selegiline
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
[PMID: 31265934]
BTI-TN-5B1-4 IC50
5.5 nM
Compound: Selegiline
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
[PMID: 30522087]
BTI-TN-5B1-4 IC50
67.25 nM
Compound: R(-)deprenyl
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
[PMID: 21872365]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: D
Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
[PMID: 23153812]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: R-(-)-deprenyl
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
[PMID: 20715818]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay
[PMID: 23927971]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method
[PMID: 22222137]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: D
Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
10.1039/C0MD00014K
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
[PMID: 23474901]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method
[PMID: 21405131]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: R-(-)-Deprenyl
Inhibition of human recombinant MAO-A expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method
Inhibition of human recombinant MAO-A expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method
[PMID: 21316817]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: (R)-(-)-Deprenyl
Inhibition of human recombinant MAO-A expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
Inhibition of human recombinant MAO-A expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
[PMID: 24746464]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production
[PMID: 25532905]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: Selegiline
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
[PMID: 27135371]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: (R)(-)D
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay
[PMID: 20045650]
BTI-TN-5B1-4 IC50
67.25 μM
Compound: (R)-(-)-deprenyl
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method
Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method
[PMID: 19267475]
BTI-TN-5B1-4 IC50
67250 nM
Compound: R-(-)-deprenyl
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
[PMID: 20579890]
BTI-TN-5B1-4 IC50
68.73 μM
Compound: Deprenyl
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay
[PMID: 22005185]
HEK293 IC50
> 500 μM
Compound: L-Deprenyl
Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
Inhibition of human recombinant BuChE expressed in HEK293 cells using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
[PMID: 26471320]
HEK293 IC50
> 500 μM
Compound: L-Deprenyl
Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman's method
[PMID: 26471320]
体外研究
(In Vitro)

Selegiline (1 nM-1 μM) inhibits recombinant human MAO-B in a concentration-dependent manner[1].
Selegiline (10 mM) increases the efflux of norepinephrine (NE), dopamine (DA) and serotonin (5-HT) from the rat hypothalamus in vitro. Selegiline inhibits the efflux of dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA) in a dose-dependent manner[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Selegiline (1 mg/kg; i.p. daily for 24 days) reduces Cocaine self-administration of mice and does not affect Cocaine-caused body weight loss. Selegiline reduces 3,4-dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA) concentrations in frontal cortex[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice (20-22 g)[4]
Dosage: 1 mg/kg
Administration: I.p. daily for 24 days
Result: Single injection did not acutely affect mouse locomotor activity.
14 consecutive days administration did not affect food reward.
Reduced Cocaine self-administration, and reduced DOPAC and 5-HIAA concentrations in frontal cortex.
分子量

187.28

Formula

C13H17N

CAS 号
中文名称

司来吉兰

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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目录号:
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