Chemical Name: 4-[[6-Methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]benzonitrile
Biological ActivityPotent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation.
Felder et al.
Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle.
Holland et al.
Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.
Life Sci., 2005;76:1307
Citations for LY 320135
The citations listed below are publications that use Tocris products. Selected citations for LY 320135 include:
4 Citations: Showing 1 - 4
Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
Authors: Stanley Et al.
J Neurosci 2015;107:568
HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity.
Authors: Vicente-Sánchez Et al.
Mol Brain 2013;6:42
Modulation of network oscillatory activity and GABAergic synaptic transmission by CB1 cannabinoid receptors in the rat medial entorhinal cortex.
Authors: Morgan Et al.
Neural Plast 2008;2008:808564
Cannabinoid action in the olfactory epithelium.
Authors: Czesnik Et al.
Proc Natl Acad Sci U S A 2007;104:2967
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