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1-(2,4-二氯苯基)-5-(4-甲氧基苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺

用途

NIDA-41020是一种有效的选择性大麻素受体1(CB1)拮抗剂,Ki为4.1nM。NIDA-41020被设计为一种潜在的放射性配体,用于正电子发射断层扫描(PET)[1]。

名称

[ CAS 号 ]:
502486-89-7

[ 中文名 ]:
1-(2,4-二氯苯基)-5-(4-甲氧基苯基)-4-甲基-N-(1-哌啶基)-1H-吡唑-3-甲酰胺

[ 英文名 ]:
NIDA-41020

[英文别名 ]:

Roxindole hydrochloride

生物活性

[ 描述 ]:

NIDA-41020是一种有效的选择性大麻素受体1(CB1)拮抗剂,Ki为4.1nM。NIDA-41020被设计为一种潜在的放射性配体,用于正电子发射断层扫描(PET)[1]。

[ 相关类别 ]:

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 大麻素受体

[ 靶点 ]

CB1:4.1 nM (Ki)

[参考文献]

[1]. Katoch-Rouse R, et al. Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity. J Med Chem. 2003 Feb 13;46(4):642-5.

物理化学性质

[ 分子式 ]:
C₂₃H₂₄Cl₂N₄O₂

[ 分子量 ]:
459.36800

[ 精确质量 ]:
458.12800

[ PSA ]:
59.39000

[ LogP ]:
5.62260

[ 外观性状 ]:
固体

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H315-H319-H335

[ 警示性声明 ]:
P261-P264-P301 + P310-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 风险声明 (欧洲) ]:
25-36/37/38

[ 安全声明 (欧洲) ]:
26-45

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

文献

Keynote review: Medicinal chemistry strategies to CB1 cannabinoid receptor antagonists

Drug Discov. Today 10 , 693-702, (2005)

The proven clinical efficacy of the CB1 cannabinoid receptor antagonist rimonabant in obesity and its further therapeutic potential has given a tremendous impetus to the discovery of novel CB1 antagon...

Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.

J. Med. Chem. 46 , 642-645, (2003)

Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in...

更多文献