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。
| 生物活性 | ADX-47273 is a potent, selective and brain-penetrantmGluR5positive allosteric modulator (PAM), with anEC50of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities[1][2]. |
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体外研究
(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[1].
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 EC50of 0.23 μM[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a Kiof 4.3 μM[1].
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体内研究
(In Vivo) | ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex[1].
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice[1].
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[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice[3].
| Animal Model: | Male Long-Evans rats[1] | | Dosage: | 1, 10 mg/kg | | Administration: | A single i.p. | | Result: | Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 31 mg/mL(83.93 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.7074 mL | 13.5369 mL | 27.0739 mL | | 5 mM | 0.5415 mL | 2.7074 mL | 5.4148 mL | | 10 mM | 0.2707 mL | 1.3537 mL | 2.7074 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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