Synonyms: 6-Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl-1H-indole; 6-Methyl-3-[2-nitro-1-(2-thienyl)ethyl]-2-phenyl-1H-indole; ZCZ 011; ZCZ-011
Molecular Formula: C21H18N2O2S
Molecular Weight: 362.44
Linear Structural Formula: C21H18N2O2S
MDL Number: MFCD31692973
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: ZCZ011 is a brain-penetrant, cannabinoid receptor CB1-selective positive allosteric modulator (PAM) that enhances orthosteric agonist CP55,940, while reduces orthosteric inverse agonist SR141716A, CB1 binding. ZCZ011 potentiates AEA-stimulated GTPgammaS binding (Emax = 46.5% without vs. 115.2% with 100 nM ZCZ011; mouse brain membranes) and cellular signaling (beta-arrestin Emax = 100% without vs.157% with 100 nM ZCZ011, pERK pIC50 = 6.5 without vs. 8.3 with 10 nM ZCZ011; hCB1 cells). ZCZ011 exhibits antinociceptive efficay in murine chronic constriction injury (CCI) model of neuropathic pain & carrageenan model of inflammatory pain (40 mg/kg i.p.) without cannabimimetic side-effects.