1231220-79-3

1231220-79-3 structure

Name: LY2828360
Chemical Name: Ly-2828360
CAS Number: 1231220-79-3
Molecular Formula: C₂₂H₂₇ClN₆O
Molecular Weight: 426.942
Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
Create Date: 2019-01-20 02:03:10
Modify Date: 2024-01-05 13:11:47
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

Name	Ly-2828360
Synonyms	9H-Purine, 8-(2-chlorophenyl)-2-methyl-6-(4-methyl-1-piperazinyl)-9-(tetrahydro-2H-pyran-4-yl)- Ly-2828360 8-(2-Chlorophenyl)-2-methyl-6-(4-methyl-1-piperazinyl)-9-(tetrahydro-2H-pyran-4-yl)-9H-purine

Description	LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor Research Areas >> Neurological Disease
Target	CB2[1].
In Vivo	In WT mice, acute systemic administration of LY2828360 suppresses paclitaxel-induced mechanical and cold allodynia in a dose-dependent manner. LY2828360 produces time-dependent suppressions of paclitaxel-evoked mechanical and cold hypersensitivities and suppression of allodynia is maintained for at least 4.5 h post-injection relative to drug pre-injection levels. At 24 h post-injection, paclitaxel-induced mechanical allodynia has returned to drug pre-injection levels of hypersensitivity. Residual suppression of cold allodynia was absent by 72 h post LY2828360 treatment. Previously chronic administration of LY2828360 blocks the development of tolerance to the antiallodynic effects of morphine in WT but not in CB2KO mice. Chronic LY2828360 treatment suppresses paclitaxel-induced mechanical and cold allodynia in WT mice but not in CB2KO mice previously render tolerant to morphine[1].
References	[1]. Lin X, et al. Slowly Signaling G Protein-Biased CB2 Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence. Mol Pharmacol. 2018 Feb;93(2):49-62.