GAT211

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].

Product Specifications

CAS Number

[102704-40-5]

UNSPSC

12352005

Target

Cannabinoid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gat211.html

Purity

99.98

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=[N+]([O-])CC(C1=CC=CC=C1)C2=C(NC3=C2C=CC=C3)C4=CC=CC=C4

Molecular Formula

C22H18N2O2

Molecular Weight

342.39

References & Citations

[1]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. |[2]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.|[3]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) .