AM4113

A CB1 receptor neutral antagonist

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库存: 现货

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1mg

￥200.00

160.00

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5mg

￥925.00

740.00

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10mg

￥1537.00

1230.00

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25mg

￥3562.00

2850.00

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货号: ajci14428
CAS: 614726-85-1
别名: AM4113
分子式: C17H12Cl3N3O
分子量: 380.7
纯度: >98%
溶解度: ≤0.5mg/ml in ethanol;3mg/ml in DMSO;10mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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.