5.04275

CB1 antagonist AM251

• Synonym(s): CB1 antagonist AM251, N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide, AM 251
• Empirical Formula (Hill Notation): C₂₂H₂₁Cl₂IN₄O
• CAS Number: 183232-66-8
• Molecular Weight: 555.24
• MDL number: MFCD01861181
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 10 mg/mL
• storage temp.: 10-30°C
• InChI: 1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30)
• InChI key: BUZAJRPLUGXRAB-UHFFFAOYSA-N

Description

General description

A potent and highly selective antagonist for cannabinoid subtyre 1 (CB₁) receptor. Affinity for CB1 (IC₅₀ = 8 nM, K_i = 7.49 nM) is more than 306-fold higher than that for CB₂ receptors. Has been used in a study to determine its interaction with hippocampal neurons to enhance spatial memory in mice.

Biochem/physiol Actions

Primary Target
CB₁ Receptor

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Gatley, S., et al. 1996. Eur. J. Pharmacol.307, 331.
Gatley, S., et al. 1997. Life Sci.61, 191.
Lan, R., et al. 1999. J. Med. Chem.42, 769.
Pertwee, R., 2005. Life Sci.76, 1307.

Ryberg, E., et al. 2007. Br. J. Pharmacol.152, 1092.
Assini, F., et al. 2012. Behav. Pharmacol.23, 292.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(C): Not applicable