LY2828360

LY2828360

Identifiers
IUPAC name 8-(2-chlorophenyl)-2-methyl-6-(4-methylpiperazin-1-yl)-9-(oxan-4-yl)purine
CAS Number	1231220-79-3
PubChem CID	46833780
DrugBank	DB16074
ChemSpider	31104907
UNII	O12H7VFU6P
ChEMBL	ChEMBL3139186
Chemical and physical data
Formula	C22H27ClN6O
Molar mass	426.95 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=NC2=C(C(=N1)N3CCN(CC3)C)N=C(N2C4CCOCC4)C5=CC=CC=C5Cl
InChI InChI=1S/C22H27ClN6O/c1-15-24-21(28-11-9-27(2)10-12-28)19-22(25-15)29(16-7-13-30-14-8-16)20(26-19)17-5-3-4-6-18(17)23/h3-6,16H,7-14H2,1-2H3 Key:UCMNDPDJRSEZPL-UHFFFAOYSA-N

LY2828360 is a drug which acts as a potent, selective and long acting agonist of the cannabinoid CB₂ receptor. It was effective against neuropathic pain and allodynia in animal models, but was unsuccessful in human clinical trials against arthritis pain. ^{[1] [2] [3] [4]}

References

1. Lin X, Dhopeshwarkar AS, Huibregtse M, Mackie K, Hohmann AG (February 2018). "Slowly Signaling G Protein-Biased CB₂ Cannabinoid Receptor Agonist LY2828360 Suppresses Neuropathic Pain with Sustained Efficacy and Attenuates Morphine Tolerance and Dependence". Molecular Pharmacology. 93 (2): 49–62. doi:10.1124/mol.117.109355. PMC   5749492 . PMID   29192123.
2. Iyer V, Slivicki RA, Thomaz AC, Crystal JD, Mackie K, Hohmann AG (November 2020). "The cannabinoid CB₂ receptor agonist LY2828360 synergizes with morphine to suppress neuropathic nociception and attenuates morphine reward and physical dependence". European Journal of Pharmacology. 886 173544. doi:10.1016/j.ejphar.2020.173544. PMC   7694697 . PMID   32896549.
3. Zavala CA, Thomaz AC, Iyer V, Mackie K, Hohmann AG (October 2021). "Cannabinoid CB₂ Receptor Activation Attenuates Fentanyl-Induced Respiratory Depression". Cannabis and Cannabinoid Research. 6 (5) can.2020.0059: 389–400. doi:10.1089/can.2020.0059. PMC   8612411 . PMID   33998863.
4. Guenther KG, Wirt JL, Oliva I, Saberi SA, Crystal JD, Hohmann AG (March 2025). "The cannabinoid CB₂ agonist LY2828360 suppresses neuropathic pain behavior and attenuates morphine tolerance and conditioned place preference in rats". Neuropharmacology. 265 110257. doi:10.1016/j.neuropharm.2024.110257. PMC  11729772. PMID   39644993.