LY320135 

LY320135 is a potent and selective antagonist of CB1 receptor, with a K_i of 141 nM. LY320135 also binds to 5-HT₂ and muscarinic receptors with K_is of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect^[1][2].

LY320135 has a relatively low affinity for the CB2 receptor (K_i=14.9±0.4 μM) and ten other unrelated receptors^[1].
LY320135 (1 nM-10 μM) inhibits the anandamide-mediated forskolin-stimulated cAMP accumulation in CHO cell, with an IC₅₀ of 734±122 nM^[1].
LY320135 (0.1-1000 nM; 1-8 min) can reverse calcium current (I_Ca) inhibition by WIN 55212-2 in N18 cells, with an IC₅₀ of 55±10 nM^[1].
LY320135 (1 μM) prevents activation of K_ir current by WIN 55212-2 in AtT-20-CB1 cells^[1].
LY 320135 (0.001-1 μM) reduces CA1 injury induced by 20 min oxygen-glucose deprivation (OGD) in a concentration-dependent manner^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

383.40

C₂₄H₁₇NO₄

176977-56-3

N#CC1=CC=C(C(C2=C(C3=CC=C(OC)C=C3)OC4=CC(OC)=CC=C24)=O)C=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Felder CC, et, al. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan; 284(1):291-7.  [Content Brief]

  [2]. Landucci E, et, al. CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices. Neuropharmacology. 2011 Mar; 60(4):674-82.  [Content Brief]