Chemical Structure : AM251
CAS No.: 183232-66-8
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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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.
M.Wt | 555.24 | |
Formula | C22H21Cl2IN4O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide |
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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