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TM 38837 New
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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 617.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||8.1 mL||40.49 mL||80.97 mL|
|1 mM||1.62 mL||8.1 mL||16.19 mL|
|2 mM||0.81 mL||4.05 mL||8.1 mL|
|10 mM||0.16 mL||0.81 mL||1.62 mL|
References are publications that support the biological activity of the product.
Hung et al (2010) 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. Chem.Med.Chem. 5 1439 PMID: 20652930
Takano et al (2014) Low brain CB1 receptor occupancy by a second generation CB1 receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: a PET study. Synapse. 68 89 PMID: 24293119
Micale et al (2019) The cannabinoid CB1 antagonist TM38837 with limited penetrance to the brain shows reduced fear-promoting effects in mice. Front.Pharmacol. 10 PMID: 30949045
If you know of a relevant reference for TM 38837, please let us know.
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Keywords: TM 38837, TM 38837 supplier, TM38837, cannabinoid, CB1, receptor, inverse, agonist, highly, potent, peripherally, restricted, Receptors, 7131, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.