LY 320135
Chemical Name: 4-[[6-Methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]benzonitrile
Purity: ≥98%
Biological Activity
LY 320135 is a potent 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).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation.
Felder et al.
J.Pharmacol.Exp.Ther., 1998;284:291 -
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.
Br.J.Pharmacol., 1999;128:597 -
Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.
Pertwee
Life Sci., 2005;76:1307
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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
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Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
Authors: Stanley Et al.
J Neurosci 2015;107:568
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HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity.
Authors: Vicente-Sánchez Et al.
Mol Brain 2013;6:42
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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
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Cannabinoid action in the olfactory epithelium.
Authors: Czesnik Et al.
Proc Natl Acad Sci U S A 2007;104:2967
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