LY320135

LY320135 is a selective small molecule antagonist and inverse agonist of the cannabinoid CB1 receptor. Developed by Eli Lilly, it has been extensively utilized as a pharmacological tool to investigate the role of the endocannabinoid system in various physiological and pathological processes. Research has demonstrated its ability to modulate frontocortical neurotransmitter release (including glutamate and serotonin), hippocampal synaptic transmission, and circadian activity rhythms. Unlike some other CB1 antagonists such as rimonabant or AM251, LY320135 has been reported to lack significant off-target positive allosteric modulation of GABA(A) receptors at standard experimental concentrations. Additionally, preclinical studies have explored its potential neuroprotective effects in models of transient focal cerebral ischemia and its ability to block certain non-CB1/CB2 mediated effects of other cannabinoid ligands.

Other names

[6-methoxy-2-(4-methoxyphenyl)benzo[b]thien-3-yl](4-cyanophenyl)methanone4-[6-methoxy-2-(4-methoxyphenyl)benzofuran-3-carbonyl]benzonitrile