| Bioactivity | 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]. |
| Invitro | 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]. |
| Name | LY320135 |
| CAS | 176977-56-3 |
| Formula | C24H17NO4 |
| Molar Mass | 383.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |