LY 320135

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Cat.No. 2387 - LY 320135 | C24H17NO4 | CAS No. 176977-56-3
Description: Selective CB1 receptor antagonist/inverse agonist
Chemical Name: 4-[[6-Methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]benzonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.5 30

Preparing Stock Solutions

The following data is based on the product molecular weight 383.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.61 mL 13.04 mL 26.08 mL
5 mM 0.52 mL 2.61 mL 5.22 mL
10 mM 0.26 mL 1.3 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Selective, CB1, receptor, antagonists, inverse, agonists, cannabinoids, Receptors, LY320135, cb1r, CB1, Receptors, Tocris Bioscience

4 Citations for LY 320135

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

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

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

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

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


Do you know of a great paper that uses LY 320135 from Tocris? If so please let us know.

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