- ￥2120 - 12400
- TargetMol
- T10168
- 2026年07月07日
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- CAS号：
142477-34-7
- 规格：
1mg/5mg/10mg/25mg/50mg
| 规格： | 1mg | 产品价格： | ￥2120.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥4640.0 |
| 规格： | 10mg | 产品价格： | ￥6144.0 |
| 规格： | 25mg | 产品价格： | ￥9200.0 |
| 规格： | 50mg | 产品价格： | ￥12400.0 |
Product Introduction
Bioactivity
| 名称 | 5-HT1A modulator 1 |
| 描述 | 5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia. |
| 激酶实验 | Binding was determined using membranes prepared from bovine hippocampus. Receptors were labeled with 0.5 nM [3H]-8-OH-DPAT by incubating with 11 concentrations of test compounds (1-10^5 nM) for 30 min at 25°C. Nonspecific binding was determined using 10 μM buspirone. Competition experiments were analyzed using the iterative nonlinear least squares curve fitting program Inplot 4, GraphPad. IC50 values were calculated using the Cheng-Prusoff equation. |
| 动物实验 | Inject Swiss mice with test compounds (e.g. 5-HT1A modulators 1, 0.25 and 1 mg/kg i.p) prior to injection of 5-HTP (400 mg/kg i.p). Count the number of head twitches that occurred during the 10 minutes starting 10 minutes after the injection of 5HTP. Cyproheptadine was used as reference compound. Wistar rats (n=6) were used. 5-HT1A Modulator 1 was tested at pharmacological doses (1 and 2 mg/kg i.p) and high doses (32 and 64 mg/kg i.p). The intensity of forepaw pedaling was expressed as a percentage of the maximum possible score. The 5-HT1A agonist 8-OH-DPAT induced forepaw trampling and was used as a reference compound. |
| 体外活性 | 方法： 采用放射性配体结合实验，在表达相应受体的细胞中检测5-HT1A modulator 1 (化合物24) 对5HT1B、5-HT2A和5-HT2C受体的亲和力。 结果： 5-HT1A modulator 1对5HT1B、5-HT2A和5-HT2C受体显示出亲和力，IC50值分别为300±55 nM、500±75 nM和4000±440 nM。[1] |
| 体内活性 | 方法： 采用小鼠模型，腹腔注射5-HT1A modulator 1（1 mg/kg），检测其对5-HT2A亚型的拮抗作用及对定型行为和攀爬行为的影响；采用大鼠模型，口服给予5-HT1A modulator 1（2、4、8、16 mg/kg），检测其拮抗作用及对过动行为的影响。 结果： 在小鼠中，5-HT1A modulator 1表现出对5-HT2A亚型94%的拮抗作用，并完全阻断定型行为和攀爬行为。在大鼠中，2 mg/kg和4 mg/kg剂量下分别显示63%和58%的拮抗作用；8 mg/kg和16 mg/kg剂量下拮抗作用完全（分别为103%和108%），并显著减少50%的过动行为。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 5 mg/mL (13.04 mM), Sonication is recommended. |
| 关键字 | α1-adrenergic receptor | α1 receptor | sPLA2 | DopamineReceptor | Dopamine Receptor | D2 receptor | AdrenergicReceptor | Adrenergic Receptor | 5HTReceptor | 5-HT2C Receptor | 5-HT2C | 5-HT2A Receptor | 5-HT2A | 5-HT1B Receptor | 5-HT1B | 5-HT1A modulator 1 | 5-HT1A | 5HT Receptor |
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| 相关库 | Lipid Metabolism Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Alzheimer's Disease Compound Library | Neurotransmitter Receptor Compound Library | Adrenergic Receptor-Targeted Compound Library | Neuronal Signaling Compound Library | Anti-Cardiovascular Disease Compound Library | GPCR Compound Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library |
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文献和实验Protein Kinase C as a Modulator of 5- HT1A and Dopamine- D2 Receptor Signaling
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Dendritic Cell Development from Mobilized Peripheral Blood CD34+Cells
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