Chemical Name:[(3S)-2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrro
lo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenyl-methan
one monomethanesulfonate
Biological Activity:
Novel, low potency CB2 receptor silent antagonist and
CB1 receptor partial inverse agonist. Competitively antagonises
effects of CP 55,940 (pA2 = 6.1) and SR 144528 (pEC50 =
5.3) at CB2 receptors and acts as a partial inverse agonist at CB1
receptors (pIC50 = 5.5). Displays modest activity at human
melatonin MT1 and muscarinic M4 receptors, but is
selective over several other GPCRs.
Savinainenet al (2005) Identification of WIN55212-3 as a
competitive neutral antagonist of the human cannabinoid CB2
receptor. Br.J.Pharmacol. 145 636.
Highly selective CB2 receptor agonist; Ki values are 0.037 and 363 nM for CB2 and CB1 receptors respectively. Increases P-ERK1/2 expression in HL-60 cells in vitro.