| Chemical Properties | Back Directory | [Melting point ]
171-172 °C | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 41.67 mg/mL (67.48 mM) | [form ]
Solid | [pka]
11.17±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
CB1 antagonist 4 (compound 8) is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. CB1 antagonist 4 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. CB1 antagonist 4 reduces propensity for psychiatric side effects[1][2]. | [Biological Activity]
TM38837 is a peripherally selective cannabinoid receptor type 1 (CB1) receptor antagonist. It has limited brain penetration to minimize or prevent CNS adverse effects and retain potential anti-obesity effects. Also it can reduces the propensity for psychotic side effects. | [in vivo]
TM38837 (10-100 mg/kg; po) induces a significant increase in freezing behavior at 100 mg/kg. | Animal Model: | < td class="col2"> 7-8 weeks old male C57BL/6 N mice (B6N) | Dosage: | 10, 30, or 100 mg/kg | | Administration: | po < /td> | | Result: | High dose (100 mg/kg) induced a significant increase in freezing behavior. < /td> | | [target]
| [IC 50]
CB1 | [storage]
Store at -20°C | [References]
[1] Micale V, et al. The Cannabinoid CB1 Antagonist TM38837 With Limited Penetrance to the Brain Shows ReducedFear-Promoting Effects in Mice. Front Pharmacol. 2019 Mar 20;10:207. DOI:10.3389/fphar.2019.00207
[2] Klumpers LE, et al. Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects. Br J Clin Pharmacol. 2013 Dec;76(6):846-57. DOI:10.1111/bcp.12141 |
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