For research use only. Not for therapeutic Use.
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research[1].
GAT211 is stable in both human- and rat-liver microsomal incubations, with t1/2 of 28.4 min and 8.67 min, repsectively[2].GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation in Neuro2a cells[3].
GAT211 potentiates the inhibition of electrically evoked vas deferens contraction in the same system (EC50=11 nM, Emax=70)[2]. GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 mL/kg; ip; 2 doses with 5 min interval) dose-dependently reduced locomotor activity and the acoustic startle response.GAT211 is dissolved in a vehicle of ethanol, kolliphor, and saline at a ratio of 1:1:6 and injected at a volume of 5 mL/kg[3].
| Catalog Number | I027956 |
| CAS Number | 102704-40-5 |
| Synonyms | 3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole |
| Molecular Formula | C22H18N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2 |
| InChIKey | OHZDCJJHWPHZJD-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(C[N+](=O)[O-])C4=CC=CC=C4 |
| Reference | [1]. Garai S, et al. Design, synthesis, and pharmacological profiling of cannabinoid 1 receptor allosteric modulators: Preclinical efficacy of C2-group GAT211 congeners for reducing intraocular pressure. Bioorg Med Chem. 2021 Nov 15;50:116421. [2]. McElroy DL, et al. Antipsychotic potential of the type 1 cannabinoid receptor positive allosteric modulator GAT211: preclinical in vitro and in vivo studies. Psychopharmacology (Berl). [3]. Richard A Slivicki, et al. Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or Dependence. Biol Psychiatry. 2018 Nov 15;84(10):722-733. |
