Chemical Name: 1-(2,4-Dichlorophenyl)-4-ethyl-N-1-piperidinyl-5-[5-[2-[4-(trifluoromethyl)phenyl]ethynyl]-2-thienyl]-1H-pyrazole-3-carboxamide
Biological ActivityTM 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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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.
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.
The cannabinoid CB1 antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice.
Micale et al.
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