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ADX-47273

CAS No. : 851881-60-2

MCE 站：ADX-47273

产品活性：ADX-47273 是一种有效的，选择性和可透过血脑屏障的 mGluR5 阳性变构调节剂 (PAM)，增强谷氨酸 (50 nM) 反应的 EC₅₀ 值为 0.17 μM。 ADX-47273 具有抗精神病和增强认知的活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself.
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC₅₀ of 0.23 μM.
ADX47273 (0.01-10 μM; 60 min) inhibits [³H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a K_i of 4.3 μM.

In Vivo: ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex.
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats.
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice.
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats.
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice.

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