2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor Dopamine Transporter Adrenergic Receptor
  4. CYD-1-79

CYD-1-79 是一种选择性的 5-HT2C 受体正向变构调节剂。CYD-1-79 通过一个拓扑学上独特的变构位点增强 5-羟色胺 (5-HT) 诱导的细胞内钙释放。CYD-1-79 对多巴胺 D3 受体、DAT 及 α2A/α2B 肾上腺素能受体的结合表现出显著抑制作用CYD-1-79 可调节啮齿类动物中 5-HT2C 受体介导的自主活动，并与低剂量 5-HT2C 受体激动剂产生协同作用。CYD-1-79 可在啮齿类动物自身给药模型中降低精神活性物质的复吸易感性。CYD-1-79 可用于神经系统疾病的研究。

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CYD-1-79

CYD-1-79 Chemical Structure

CAS No. : 2220235-94-7

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CYD-1-79 相关抗体

Top Publications Citing Use of Products

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease[1].

IC50 & Target[1]

5-HT2C Receptor

 

D3 Receptor

 

Alpha-2A adrenergic receptor

 

Alpha-2B adrenergic receptor

 

体外研究
(In Vitro)

CYD-1-79 (Compound 16) (1 pM-1 μM; 15 min) 在多种浓度下均可促进 5-羟色胺诱发的钙离子释放量上调，且未出现左移现象[1]。
CYD-1-79 (1 pM-1 μM; 15 min) 不调控 h5-HT2A R-CHO 细胞中由 5-HT2A 受体介导的细胞内钙释放，体现出对 5-HT2C 受体的亚型选择性[1]。
CYD-1-79 (10 μM) 对 5-HT 受体亚型 (包括 5-HT2C) 的正构结合位点无显著结合作用，但对多巴胺 D3 受体、DAT 及 α2A/α2B 肾上腺素能受体的结合表现出显著抑制作用[1]。

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

CYD-1-79 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-inf F CL Vss
Rat[1] 5 mg/kg i.v. 6.59 ± 0.26 h / / 939 ± 108 ng·h/mL / 5.37 ± 0.61 L/h/kg 35.07 ± 4.66 L/kg
Rat[1] 10 mg/kg p.o. 5.82 ± 0.37 h 3.3 ± 0.58 h 68.1 ± 6.8 ng/mL 737 ± 56 ng·h/mL 39.1 % / /
体内研究
(In Vivo)

CYD-1-79 (Compound 16)(0.5-5 mg/kg；腹腔注射；单次给药) 可在给药后前 30 分钟内，以 5 mg/kg 剂量显著抑制雄性 Sprague-Dawley 大鼠的自主水平及垂直活动，而较低剂量则无显著效应[1]。
CYD-1-79 (5 mg/kg；腹腔注射；单次给药) 可变构增强 5-HT2C 激动剂 WAY163909 (HY-15401) 对雄性 Sprague-Dawley 大鼠的运动抑制作用，该效应由 5-HT2C 受体激活介导[1]。
CYD-1-79 (0.125-1 mg/kg；腹腔注射，单次给药) 单独给药时可部分替代 5-HT2C 激动剂 WAY163909 的辨别刺激效应，但与低剂量 WAY163909 (0.5 mg/kg) 联用时，可在经过训练的雄性 Sprague-Dawley 大鼠中完全替代其辨别刺激效应[1]。
CYD-1-79 (compound 16) (1 mg/kg；腹腔注射；单次给药) 可显著抑制经训练自主摄入精神活性物质的雄性 Sprague-Dawley 大鼠对精神活性物质线索的反应性[1]。

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

Animal Model: Sprague-Dawley (male, 225-325 g)[1]
Dosage: 0.5 mg/kg; 1 mg/kg; 5 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced mean total ambulations and mean total vertical activity (±SEM) compared to saline at 5 mg/kg (p < 0.05).
Did not produce statistically significant changes in ambulations or vertical activity relative to saline at 0.5 mg/kg and 1 mg/kg.
Animal Model: Sprague-Dawley (male, 250-275 g, trained to self-administer psychoactive substance)[1]
Dosage: 1 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced presses on the previously active lever during the 60-minute cue-reinforced component compared to vehicle (p < 0.05, with significant differences observed at multiple 5-minute time points).
Did not significantly alter inactive lever presses relative to vehicle.
分子量

356.54

Formula

C20H40N2O3
CAS 号
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

CYD-1-79 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYD-1-792220235-94-75-HT ReceptorDopamine ReceptorDopamine TransporterAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorDATSLC6A3Beta Receptor5-HT2A receptorh5-HT2A R-CHO cellsdopamine D3 receptorα2A adrenergic receptorsh5-HT2C R-CHO cells5-HT2C receptorintracellular calcium releaseα2B adrenergic receptorscocaine use disorderInhibitorinhibitorinhibit

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