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ADX71743

CAS No. : 1431641-29-0

MCE 站：ADX71743

产品活性：ADX71743 是一种高度选择性，非竞争性且透过血脑屏障的代谢型谷氨酸受体 7 负变构调节剂 (mGlu7 NAM)。ADX71743 具有抗焦虑活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: ADX71743 has an IC₅₀ of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction.
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal.
ADX71743 can against an EC₈₀ of glutamate (IC₅₀ of 22 nM) as well as against an EC₈₀ of L-AP4 (IC₅₀ of 125 nM).

In Vivo: ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T_1/2 of 0.68, 0.40 hours, a C_max of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.

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