AM 281

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CB₁ receptor ligand

Analog of the cannabinoid receptor (CB) antagonist SR 141716A. Potent CB₁ receptor antagonist/inverse agonist (K_i=14nM).

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Alternative Name	1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
Appearance	White to off-white solid.
CAS	202463-68-1
Couple Target	Cannabinoid receptor
Couple Type	Ligand
Formula	C₂₁H₁₉Cl₂IN₄O₂
Identity	Identity determined by 1H-NMR.
MW	557.2
Purity	≥98% (HPLC)
Solubility	Soluble in methanol (1mg/ml) or DMSO (2mg/ml at RT, 50mg/ml in hot DMSO, after cooling this solution is stable over several days.)

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Effects of AM281, a cannabinoid antagonist, on systemic haemodynamics, internal carotid artery blood flow and mortality in septic shock in rats: Y. Kadoi, et al.; Br. J. Anaesth. 94, 563 (2005), Abstract
Cannabinoid antagonist AM 281 reduces mortality rate and neurologic dysfunction after cecal ligation and puncture in rats: Y. Kadoi, et al.; Crit. Care Med. 33, 2629 (2005), Abstract
Effects of the cannabinoid antagonists AM281 and AM630 on deprivation-induced intake in Lewis rats: N.A. Werner, et al.; Brain Res. 967, 290 (2003), Abstract
Large receptor reserve for cannabinoid actions in the central nervous system: A. N. Gifford, et al.; J. Pharmacol. Exp. Ther. 288, 478 (1999), Abstract
Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo: S.J. Gatley, et al.; J. Neurochem. 70, 417 (1998), Abstract
Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices: A.N. Gifford, et al.; Neurosci. Lett. 238, 84 (1997), Abstract

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