LY 320135

Discontinued Product

LY 320135 (Cat. No. 2387) has been withdrawn from sale for commercial reasons.
Description: Selective CB1 inverse agonist
Chemical Name: 4-[[6-Methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]benzonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews
Literature (2)

Biological Activity for LY 320135

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 for LY 320135

M. Wt 383.4
Formula C24H17NO4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 176977-56-3
PubChem ID 5311257
InChI Key RYNSGDFWBJWWSZ-UHFFFAOYSA-N
Smiles COC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(C=C2)C#N)C2=CC=C(OC)C=C2O1

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.

Product Datasheets for LY 320135

Certificate of Analysis / Product Datasheet
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References for LY 320135

References are publications that support the biological activity of the product.

Felder et al (1998) LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J.Pharmacol.Exp.Ther. 284 291 PMID: 9435190

Holland et al (1999) Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Br.J.Pharmacol. 128 597 PMID: 10516638

Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307 PMID: 15670612

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Keywords: LY 320135, LY 320135 supplier, Selective, CB1, receptor, antagonists, inverse, agonists, cannabinoids, Receptors, LY320135, cb1r, 2387, Tocris Bioscience

4 Citations for LY 320135

Citations are publications that use Tocris products. Selected citations for LY 320135 include:

Vicente-Sánchez et al (2013) HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity. Mol Brain 6 42 PMID: 24093505

Stanley et al (2015) Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation. J Neurosci 107 568 PMID: 26092099

Czesnik et al (2007) Cannabinoid action in the olfactory epithelium. Proc Natl Acad Sci U S A 104 2967 PMID: 17301239

Morgan et al (2008) Modulation of network oscillatory activity and GABAergic synaptic transmission by CB1 cannabinoid receptors in the rat medial entorhinal cortex. Neural Plast 2008 808564 PMID: 19079598


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.