LY320135

[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]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[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.

[ 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

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ HS Code ]:
2932999099

[ 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%

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...

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