Catalog Number: 2387
Chemical Name: 4-[[6-Methoxy-2-(4-methoxyphenyl)-3-benzofuranyl]carbonyl]benzonitrile
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
  • Solubility:
    Soluble to 30 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    176977-56-3
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.
Background References
  1. 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
  2. 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
  3. Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.
    Pertwee
    Life Sci., 2005;76:1307
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LY 320135 include:

4 Citations: Showing 1 - 4
Filter your results:

  1. Cannabidiol causes endothelium-dependent vasorelaxation of human mesenteric arteries via CB1 activation.
    Authors: Stanley Et al.
    J Neurosci 2015;107:568
  2. HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity.
    Authors: Vicente-Sánchez Et al.
    Mol Brain 2013;6:42
  3. 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
  4. Cannabinoid action in the olfactory epithelium.
    Authors: Czesnik Et al.
    Proc Natl Acad Sci U S A 2007;104:2967

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