| 货号 | 13453-1mg |
| 描述 | LH 21 is a 1,2,4-triazole that acts as a cannabimimetic. It has a relatively low-affinity for the central cannabinoid (CB1) receptor (Ki = 855 nM).1 However, it interferes, at low nanomolar concentrations, with the action of the potent CB1 agonist WIN 55,212-2 on murine vas deferens, suggesting that LH 21 acts as a silent CB1antagonist.1 Consistent with this interpretation, LH 21 diminishes the in vivo effects of WIN 55,212-2 on standard CB tetrad responses in mice and reduces food intake and body weight gain in obese Zucker rats.1,2,3 However, in CHO cells overexpressing CB1, LH 21 is able to elevate cAMP, suggesting that, in this model, it acts as an inverse agonist of CB1.4 Furthermore, LH 21 suppresses food intake and body weight gain in both wild-type and CB1 receptor knockout mice, indicating that this receptor is not necessary for these effects.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jagerovic, N.,Hernandez-Folgado, L.,Alkorta, I., et al. Discovery of 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. Journal of Medicinal Chemistry 47, 2939-2942 (2004). 2.Pavon, F.J.,Bilbao, A.,Hernández-Folgado, L., et al. Antiobesity effects of the novel neutral cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole - LH 21. Neuropharmacology 51, 358-366 (2006). 3.Pavón, F.J.,Serrano, A.,Pérez-Valero, V., et al. Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: Effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats. Journal of Neuroendocrinology 20, 116-123 (2008). 4.Chen, R.Z.,Frassetto, A.,Lao, J.Z., et al. Pharmacological evaluation of LH-12, a newly discovered molecule that binds to cannabinoid CB1 receptor. European Journal of Pharmacology 584, 338-342 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 407.1 |
| 分子式 | C20H20Cl3N3 |
| CAS号 | 611207-11-5 |
| 稳定性 | ≥ 2 years |
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