| Identification | Back Directory | [Name]
ABD459 | [CAS]
1047670-51-8 | [Synonyms]
ABD459
ABD459,ABD-459
[5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazol-3-yl]-(4-methoxyphenyl)-methanone | [Molecular Formula]
C24H17BrCl2N2O2 | [MOL File]
1047670-51-8.mol | [Molecular Weight]
516.21 |
| Chemical Properties | Back Directory | [Boiling point ]
615.6±55.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 3 mg/ml; DMF:PBS(pH7.2) (1:2): 0.33 mg/ml | [form ]
A crystalline solid | [pka]
-3.35±0.10(Predicted) |
| Hazard Information | Back Directory | [Description]
ABD459 is a neutral antagonist of the central cannabinoid 1 (CB1) receptor (Ki = 8.6 nM). It inhibits food consumption in nonfasted mice without affecting motor activity. ABD459 reduces active food seeking for 5-6 hours after treatment, with no rebound after washout. ABD459 also diminishes rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep. | [Uses]
ABD459 is a CB1 receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders[1]. | [storage]
Store at -20°C | [References]
[1] Goonawardena AV, et al. Modulation of food consumption and sleep-wake cycle in mice by the neutral CB1 antagonist ABD459. Behav Pharmacol. 2015 Apr;26(3):289-303. DOI:10.1097/FBP.0000000000000108 |
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