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AM4113

 
Catalog No.
C3493
大麻素受体1(CB1)选择性中性拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 818.00
Ship with 10-15 days
10mg
¥ 1,363.00
Ship with 10-15 days
25mg
¥ 2,727.00
Ship with 10-15 days

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A

背景

AM4113, a pyrazole analog structurally related to SR141716 and AM251, is a novel cannabinoid CB1 neutral antagonist. AM4113 suppressed food intake and food-reinforced behavior in rats.

In vitro: AM4113 was able to bind with high affinity to CB1 receptors, exhibiting 100-fold selectivity for CB1 against CB2 receptors. The Ki value for CB1 was 0.897 ± 0.44 nM, while the Ki value for hCB2 was 92 ± 6.9 nM [1].

In vivo: In rats, treatment with AM4113 (2.0 and 4.0 mg/kg) attenuated the AM411-induced locomotor suppression and analgesia. In addition, 4.0 mg/kg AM4113 alone significantly suppressed locomotor activity when compared with vehicle. AM4113 dose-dependently decreased lever pressing on an FR1 schedule. AM4113 produced conditioned taste avoidance and suppression of ingestive (hedonic) taste reactivity scores in a dose-dependent manner [1]. AM4113 didn’t induce signs of nausea [1].

Reference:
[1] Sink K S, McLaughlin P J, Wood J A T, et al.  The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats[J]. Neuropsychopharmacology, 2008, 33(4): 946-955.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt380.7
Cas No.614726-85-1
FormulaC17H12Cl3N3O
Solubility≤0.5mg/ml in ethanol;3mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
SDFDownload SDF
Canonical SMILESClC1=CC(Cl)=CC=C1N2C(C3=CC=C(Cl)C=C3)=C(C)C(C(N)=O)=N2
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化学结构

AM4113