LY320135
LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
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- CAS No.: 176977-56-3
- Formule: C24H17NO4
- Masse moléculaire:383.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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CB1 141 nM (Ki) |
5-HT2 Receptor 6.4 μM (Ki) |
muscarinic receptor 2.1 μM (Ki) |
CB2 >10 μM (Ki) |
LY320135 has a relatively low affinity for the CB2 receptor (Ki=14.9±0.4 μM) and ten other unrelated receptors[1].
LY320135 (1 nM-10 μM) inhibits the anandamide-mediated forskolin-stimulated cAMP accumulation in CHO cell, with an IC50 of 734±122 nM[1].
LY320135 (0.1-1000 nM; 1-8 min) can reverse calcium current (ICa) inhibition by WIN 55212-2 in N18 cells, with an IC50 of 55±10 nM[1].
LY320135 (1 μM) prevents activation of Kir current by WIN 55212-2 in AtT-20-CB1 cells[1].
LY 320135 (0.001-1 μM) reduces CA1 injury induced by 20 min oxygen-glucose deprivation (OGD) in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 176977-56-3
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Masse moléculaire 383.40
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Formule C24H17NO4
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SMILES
N#CC1=CC=C(C(C2=C(C3=CC=C(OC)C=C3)OC4=CC(OC)=CC=C24)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Felder CC, et, al. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan; 284(1):291-7. [Content Brief]
[2]. Landucci E, et, al. CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices. Neuropharmacology. 2011 Mar; 60(4):674-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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