A cannabimimetic with a relatively low-affinity for the CB1 receptor (Ki = 855 nM); interferes with the action of the potent CB1 agonist WIN 55

LH 21 – 10 mg

Brand:
Cayman
CAS:
611207-11-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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).{19248} 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 CB1 antagonist.{19248} 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.{19248,19238,19239} 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.{19237} 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.{19237}  

 

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Description

A cannabimimetic with a relatively low-affinity for the CB1 receptor (Ki = 855 nM); interferes with the action of the potent CB1 agonist WIN 55,212-2, suggesting that it acts as a silent CB1 antagonist; reduces food intake and body weight gain in obese Zucker rats

Formal name: 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole

Synonyms: 

Molecular weight: 408.8

CAS: 611207-11-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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