1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  2. 5-HT Receptor COMT Endogenous Metabolite
  3. Serotonin

Serotonin  (Synonyms: 5-Hydroxytryptamine; 5-HT)

目录号: HY-B1473A 纯度: 99.86%
COA 产品使用指南 技术支持

Serotonin 是 CNS 中的单胺神经递质和内源性 5-HT 受体激动剂。Serotonin 也是儿茶酚 O-甲基转移酶 (COMT) 的抑制剂,其 Ki 值为 44 μM。

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Serotonin Chemical Structure

Serotonin Chemical Structure

CAS No. : 50-67-9

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Other Forms of Serotonin:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.

IC50 & Target

Microbial Metabolite

 

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
B16 IC50
> 30 μM
Compound: 17
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
[PMID: 19524439]
C6 EC50
12 nM
Compound: 5-HT
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT
[PMID: 19334715]
CHO EC50
0.7 nM
Compound: 5-HT
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
[PMID: 16458504]
CHO EC50
1 nM
Compound: 5-HT
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
[PMID: 16392798]
CHO IC50
1.2 x 10-1 μM
Compound: Serotonin
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
CHO EC50
1.5 nM
Compound: 5-HT
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader
[PMID: 15081042]
CHO EC50
1.63 nM
Compound: 5-HT
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
Agonist activity at 5HT2C receptor expressed in CHO cells by fluorescence based calcium mobilization assay
[PMID: 22381048]
CHO EC50
1.7 nM
Compound: 5-HT
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
[PMID: 15081042]
CHO EC50
11 nM
Compound: 5-HT
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader
[PMID: 15081042]
CHO EC50
150 nM
Compound: 5-HT
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 19559623]
CHO IC50
2.5 x 10-10 M
Compound: Serotonin
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
CHO EC50
25 nM
Compound: 5-HT
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
Agonist activity at human recombinant 5HT2C receptor expressed in CHO K1 cells assessed as induction of calcium mobilization by FLIPR assay
[PMID: 19646865]
CHO EC50
4.67 nM
Compound: 1
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
[PMID: 9871775]
CHO-K1 EC50
0.07 μM
Compound: Serotonin
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
Agonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell incubated for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
[PMID: 32631561]
CHO-K1 EC50
15 nM
Compound: Serotonin
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
Agonist activity at human recombinant 5HT7 receptor expressed in CHOK1 cells assessed as increase in cAMP levels by HTRF assay
[PMID: 19326916]
CHO-K1 EC50
15.33 nM
Compound: 5-HT
Agonist activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
Agonist activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
[PMID: 27487565]
CHO-K1 EC50
16 nM
Compound: 5-HT
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
Agonist activity at 5HT2A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
[PMID: 23675993]
CHO-K1 EC50
18 nM
Compound: Serotonin
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
[PMID: 31627993]
CHO-K1 EC50
39 nM
Compound: 5-HT
Agonist activity at 5HT1A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
Agonist activity at 5HT1A receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
[PMID: 23675993]
CHO-K1 EC50
4.82 nM
Compound: 5-HT
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
[PMID: 8960551]
CHO-K1 EC50
45.3 nM
Compound: Serotonin
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
Partial agonist activity at recombinant human 5-HT1A expressed in CHO-K1 cells by pathhunter beta-arrestin assay
[PMID: 32631554]
CHO-K1 EC50
47 nM
Compound: 5-HT
Agonist activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
Agonist activity at 5-HT2A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by Fluo-4 dye based FLIPR assay
[PMID: 27487565]
Flp-In-293 EC50
0.19 nM
Compound: Serotonin
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
[PMID: 31445232]
Flp-In-293 EC50
0.27 nM
Compound: Serotonin
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
[PMID: 31445232]
Flp-In-293 EC50
0.86 nM
Compound: Serotonin
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay
[PMID: 31445232]
HEK293 EC50
0.00087 μM
Compound: 5-HT, serotonin
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
[PMID: 23301527]
HEK293 EC50
0.0026 μM
Compound: 5-HT, serotonin
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as induction of intracellular calcium release measured for 90 secs by fluorescence assay
[PMID: 23301527]
HEK293 EC50
0.017 μM
Compound: 5-HT, serotonin
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
[PMID: 25073094]
HEK293 EC50
0.044 μM
Compound: 5-HT, serotonin
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
[PMID: 23301527]
HEK293 EC50
0.09 nM
Compound: 5-HT
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
[PMID: 22778800]
HEK293 EC50
0.09 nM
Compound: 1
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 19284718]
HEK293 EC50
0.1 μM
Compound: serotonin
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
Activity at SER4 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay
[PMID: 18033297]
HEK293 EC50
0.15 μM
Compound: 5-HT, serotonin
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as accumulation of IP1 incubated for 1 hr at 37 degC followed by 15 mins at RT by TR-FRET assay
[PMID: 23301527]
HEK293 EC50
0.17 nM
Compound: 5-HT
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
[PMID: 28657744]
HEK293 EC50
0.21 nM
Compound: 5-HT
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 25633969]
HEK293 EC50
0.4 nM
Compound: 5-HT
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
[PMID: 23602445]
HEK293 EC50
0.41 nM
Compound: 5-HT
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
Agonist activity at human 5HT2C receptor stably expressed in HEK293 cells co-expressing Gq assessed as induction of calcium mobilization measured at 1 sec interval for 60 secs by Fluo-4 calcium dye based FLIPR assay
[PMID: 32282200]
HEK293 EC50
0.5 nM
Compound: 1
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 19284718]
HEK293 EC50
0.5 μM
Compound: 5-HT
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells by FMP assay
[PMID: 17722904]
HEK293 EC50
0.86 nM
Compound: 5-HT
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
[PMID: 22778800]
HEK293 EC50
0.92 nM
Compound: 5-HT
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 25633969]
HEK293 EC50
1.1 nM
Compound: 5-HT
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
[PMID: 23602445]
HEK293 EC50
1.46 nM
Compound: 5-HT
Agonist activity at human 5-HT2B receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
Agonist activity at human 5-HT2B receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
[PMID: 28657744]
HEK293 EC50
1.5 nM
Compound: 5-HT
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as increase in calcium mobilization by FLIPR assay
[PMID: 23602445]
HEK293 IC50
1.8 x 10-1 μM
Compound: Serotonin
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
[PMID: 27876250]
HEK293 EC50
1.88 nM
Compound: 5-HT
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 25633969]
HEK293 EC50
2.35 nM
Compound: 5-HT
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay
[PMID: 28657744]
HEK293 IC50
260 nM
Compound: Serotonin
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
[PMID: 27997171]
HEK293 EC50
3.75 nM
Compound: 5-HT
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
[PMID: 23332346]
HEK293 EC50
5.8 nM
Compound: 1
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
[PMID: 19284718]
HEK293 EC50
5.8 nM
Compound: 5-HT
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
Agonist activity at human 5-HT7R expressed in HEK293 cells assessed as induction of cAMP levels treated for 10 mins measured after 30 mins by D2-dye based fluorescence assay
[PMID: 27475109]
HEK293 EC50
7.6 nM
Compound: 5-HT
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux measured every sec for 3 mins by FLIPR assay
[PMID: 22778800]
U2OS IC50
1.25 nM
Compound: Serotonin
Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay
Antagonist activity at recombinant human 5-HT2C expressed in human U2OS cells by pathhunter beta-arrestin assay
[PMID: 32631554]
U2OS IC50
27.9 nM
Compound: Serotonin
Antagonist activity at recombinant human 5-HT2A expressed in human U2OS cells by pathhunter beta-arrestin assay
Antagonist activity at recombinant human 5-HT2A expressed in human U2OS cells by pathhunter beta-arrestin assay
[PMID: 32631554]
体外研究
(In Vitro)

Serotonin 是中枢神经系统中的单胺类神经递质,也是内源性 5-HT 受体激动剂。Serotonin 还通过非竞争性结合儿茶酚底物结合位点来抑制儿茶酚 O-甲基转移酶 (COMT),儿茶酚 O-甲基转移酶是一种有助于调节疼痛感知的酶,其结合亲和力与儿茶酚本身的结合亲和力相当 (Ki=44 μM)。结果表明,添加 100 μM Serotonin 会降低 COMT 的反应速度[1]

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

体内研究
(In Vivo)

与接受盐水治疗的对照组相比,Serotonin 会产生强烈的超敏反应 (p<0.001)[1]
在诱发 DSS 结肠炎后,接受 Serotonin 的 IL-13-/- 小鼠的结肠 5-HT 含量显著增加,而接受载体的 IL-13-/- 小鼠的结肠 5-HT 含量则较少[2]

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

Clinical Trial
分子量

176.22

Formula

C10H12N2O

CAS 号
性状

固体

颜色

White to off-white

中文名称

5-羟色胺;血清胺

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料

纯度: 99.86%

参考文献
Cell Assay
[2]

For macrophage culture, peritoneal cavity cells are collected from WT and IL-13-/- mice with or without dextran sodium sulfate (DSS) treatment and cultured. Cells are plated at a concentration of 3.0×106 cells per millilitre, and treated with either lipopolysaccharides (LPS); (100 ng/mL) or Serotonin (10-10 M) for 24 hours. The culture supernatant are collected and stored in -80°C until determination of cytokine levels using protein array system[2].

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

Animal Administration
[2]

Dextran sodium sulfate (DSS) colitis is induced by orally administering 5% DSS in drinking water for 5 days. In a separate experiment, IL-13-/- mice are injected subcutaneously with 100 mg/kg of Serotonin (5-HTP) twice daily for 8 days beginning 3 days prior to induction of DSS colitis; whereas, the control IL-13-/- mice receive saline as vehicle. Animals are anaesthetized prior to euthanization via cervical dislocation at the conclusion of each experiment or if they reach a predetermined end point (ie, loss of ≥20% body weight and/or significant deterioration of body condition)[2].

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

参考文献
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产品名称:
Serotonin
目录号:
HY-B1473A
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