NIDA-41020

Names

[ Name ]:
NIDA-41020

[Synonym ]:
1-(2,4-Dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide
Roxindole hydrochloride

Biological Activity

[Description]:

NIDA-41020 is a potent and selective cannabinoid receptor 1(CB1) antagonist with a Ki of 4.1 nM. NIDA-41020 was designed as a potential radioligand for use in positron emission tomography (PET)[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

CB1:4.1 nM (Ki)

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₄Cl₂N₄O₂

[ Molecular Weight ]:
459.36800

[ Exact Mass ]:
458.12800

[ PSA ]:
59.39000

[ LogP ]:
5.62260

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H300-H315-H319-H335

[ Precautionary Statements ]:
P261-P264-P301 + P310-P305 + P351 + P338

[ Personal Protective Equipment ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ Risk Phrases ]:
25-36/37/38

[ Safety Phrases ]:
26-45

[ RIDADR ]:
UN 2811 6.1 / PGIII

Articles

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...