LY320135

Modify Date: 2024-01-10 22:13:36

LY320135 Structure
LY320135 structure
Common Name LY320135
CAS Number 176977-56-3 Molecular Weight 383.39600
Density 1.31g/cm3 Boiling Point 617.2ºC at 760mmHg
Molecular Formula C24H17NO4 Melting Point N/A
MSDS Chinese USA Flash Point 327.1ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of 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[1][2].

 Names

Name 4-[6-methoxy-2-(4-methoxyphenyl)-1-benzofuran-3-carbonyl]benzonitrile
Synonym More Synonyms

 LY320135 Biological Activity

Description 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[1][2].
Related Catalog
Target

CB1:141 nM (Ki)

5-HT2 Receptor:6.4 μM (Ki)

muscarinic receptor:2.1 μM (Ki)

CB2:>10 μM (Ki)

In Vitro 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].
References

[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.

[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.

 Chemical & Physical Properties

Density 1.31g/cm3
Boiling Point 617.2ºC at 760mmHg
Molecular Formula C24H17NO4
Molecular Weight 383.39600
Flash Point 327.1ºC
Exact Mass 383.11600
PSA 72.46000
LogP 5.21968
Vapour Pressure 3.64E-15mmHg at 25°C
Index of Refraction 1.664
Storage condition 2-8°C

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
RIDADR UN 2811 6.1 / PGIII
HS Code 2932999099

 Customs

HS Code 2932999099
Summary 2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles1

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Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor.

Mol. Pharmacol. 88 , 368-79, (2015)

CB1 cannabinoid receptors (CB1Rs) are attractive therapeutic targets for numerous central nervous system disorders. However, clinical application of cannabinoid ligands has been hampered owing to thei...

 Synonyms

MFCD00945878