2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. NPY Y2 antagonist 2

NPY Y2 antagonist 2 是靶向神经肽 Y (NPY) 受体 Y2 的调节剂，对人和大鼠 NPY Y2 的 pKi 值分别为 6.8 nM 和 7.2 nM，对 Y1 和 Y5 受体具有选择性，且能透过血脑屏障 (blood-brain barrier penetration)。NPY Y2 antagonist 2 可阻断 NPY Y2 受体的负反馈调节机制，增加内源性 NPY 释放并增强 Y1 受体激活，发挥调控中枢神经递质释放的活性。NPY Y2 antagonist 2 具有中等体内清除率、大鼠脑游离分数、脑/血浆比，以及脑暴露量。NPY Y2 antagonist 2 可用于情感障碍、酒精戒断诱导焦虑等相关社交焦虑等疾病领域的研究 。

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NPY Y2 antagonist 2

NPY Y2 antagonist 2 Chemical Structure

CAS No. : 1262495-12-4

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NPY Y2 antagonist 2 相关抗体

Top Publications Citing Use of Products

查看 Neuropeptide Y Receptor 亚型特异性产品:

查看所有亚型
NPY Y1 receptor NPY Y2 receptor NPY Y4 receptor NPY Y5 receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal[1].

IC50 & Target

human Y2 receptor

6.8 nM (pKi)

rat Y2 receptor

7.2 nM (pKi)

NPY Y1 receptor

 

体外研究
(In Vitro)

NPY Y2 antagonist 2 (compound 149) 在体外理化性质与代谢稳定性实验中，显示出中等肝微粒体清除率（大鼠 1.8 mL/min/g，人 0.8 mL/min/g）及 97.2% 的大鼠血脑屏障结合率[1]。

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

NPY Y2 antagonist 2 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 2 mg/kg s.c. Plasma Concentration 32 ng/g
Rat[1] 2 mg/kg s.c. Brain Concentration 73 ng/g
Rat[1] 2 mg/kg s.c. Brain-to-Plasma Ratio 2.3
体内研究
(In Vivo)

NPY Y2 antagonist 2 (compound 149) (2 mg/kg; s.c.; 单剂量) 在大鼠中表现出良好的脑渗透性和暴露量，1 小时脑/血比为 2.3，脑内最高浓度达 73 ng/g，血液最高浓度为32 ng/mL[1]。

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

Animal Model: rats (specific strain not reported)[1]
Dosage: 2 mg/kg
Administration: s.c.; single dose
Result: Effectively penetrated the blood-brain barrier, with a brain/blood ratio of 2.3 at 1 hour post-administration.
The maximum concentration (Cmax) in the brain was 73 ng/g, and the Cmax in the blood was 32 ng/mL, demonstrating its ability to distribute into the central nervous system.
分子量

536.04

Formula

C27H33ClF3N5O
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

NPY Y2 antagonist 2 相关分类

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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:

NPY Y2 antagonist 21262495-12-4Neuropeptide Y ReceptorNPY receptorratY2 receptorY5 receptorsblood-brain barrierCYP isoformsanimal modelsneurological diseaseNeuropeptide Y Y2 receptorY1 receptorshumanInhibitorinhibitorinhibit

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