Cas No.: | 176977-56-3 |
Chemical Name: | 4-(6-Methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl)benzonitrile |
Synonyms: | 4-(6-Methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl)benzonitrile;4-[[6-METHOXY-2-(4-METHOXYPHENYL)-3-BENZOFURANYL]CARBONYL]BENZONITRILE;[6-Methoxy-2-(4-methoxyphenyl)benzo[b]furan-3-yl](4-cyanophenyl)methanone;4-[6-methoxy-2-(4-methoxyphenyl)-1-benzofuran-3-carbonyl]benzonitrile;Benzonitrile,4-[[6-methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]-;LY 320135;4-[6-methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl]benzonitrile;AC1NSKBE;LY-320135;SureCN3736014;4-[6-Methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl]benzonitrile;LY320135;4-[6-Methoxy-2-(4-Methoxyphenyl)benzofuran-3-carbonyl]benzonitrile;Benzonitrile,4-[[6-Methoxy-2-(4-Methoxyphenyl)-3-benzofuranyl]carbonyl]- |
SMILES: | COC1C=CC2C(C(C3C=CC(C#N)=CC=3)=O)=C(C3C=CC(OC)=CC=3)OC=2C=1 |
Formula: | C24H17NO4 |
M.Wt: | 383.396086454391 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect[1][2]. |
Target: | CB1:141 nM (Ki) 5-HT2 Receptor:6.4 μM (Ki) muscarinic receptor:2.1 μM (Ki) CB2:>10 μM (Ki) |
In Vitro: | LY320135 has a relatively low affinity for the CB2 receptor (Ki=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 (ICa) inhibition by WIN 55212-2 in N18 cells, with an IC50 of 55±10 nM[1]. LY320135 (1 μM) prevents activation of Kir 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]. |
References: | [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. [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. |