TM 38837

Biological Activity

TM 38837 is a highly potent cannabinoid 1 receptor (CB₁) inverse agonist (IC₅₀ values are 8.5 nM and 605 nM for inhibition of [³H]-CP 55940 binding at CB₁ and CB₂ receptors, respectively). Displays 71-fold selectivity for CB₁ receptors over CB₂ receptors. Inhibits GTP binding to CB₁-overexpressing cell membranes in vitro (EC₅₀ = 18.5 nM). Peripherally restricted. Promotes fear behaviors when given by intracerebrovascular (icv) injection in mice.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist.
   Hung et al.
   Chem.Med.Chem., 2010;5:1439
2. Low brain CB₁ receptor occupancy by a second generation CB₁ receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: a PET study.
   Takano et al.
   Synapse., 2014;68:89
3. The cannabinoid CB₁ antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice.
   Micale et al.
   Front.Pharmacol., 2019;10

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