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AM251

Chemical Structure : AM251

CAS No.: 183232-66-8

AM251 (AM 251)

Catalog No.: PC-20082Not For Human Use, Lab Use Only.

AM251 (AM 251) is a potent, selective CB1 receptor antagonist (inverse agonist) with IC50 of 8 nM, Ki of 7.49 nM, displays 306-fold selectivity over CB2 receptors.

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Biological Activity

AM251 (AM 251) is a potent, selective CB1 receptor antagonist (inverse agonist) with IC50 of 8 nM, Ki of 7.49 nM, displays 306-fold selectivity over CB2 receptors.
AM251 also is a potent GPR55 agonist (EC50=39 nM) and μ-opioid receptor antagonist (Ki=251 nM).
AM251 blocked the WIN 55,212-2-induced inhibition of evoked Iinhibitory postsynaptic currents (IPSCs).
Pretreatment with AM 251 (3 mg kg(-1)) antagonized the pressor and vasoconstrictor effects of HU 210 and WIN-55212-2 in conscious rats.

Physicochemical Properties

M.Wt 555.24
Formula C22H21Cl2IN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

References

1. Gatley SJ, et al. Eur J Pharmacol. 1996 Jul 4;307(3):331-8.

2. Diana MA, et al. J Neurosci. 2002 Jan 1;22(1):200-8.

3. Gardiner SM, et al. Br J Pharmacol. 2002 Jun;136(4):581-7.

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