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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
|Storage||Store at RT|
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.
Solubility Data for LY 320135
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for LY 320135
The following data is based on the product molecular weight 383.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.3 mM||8.69 mL||43.47 mL||86.94 mL|
|1.5 mM||1.74 mL||8.69 mL||17.39 mL|
|3 mM||0.87 mL||4.35 mL||8.69 mL|
|15 mM||0.17 mL||0.87 mL||1.74 mL|
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:
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
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
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Literature in this Area
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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.