MS21570

MS21570是GPR171的选择性拮抗剂，其IC50值为220nM.

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库存: 现货

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数量
10mg

￥975.00

780.00

- +
50mg

￥2912.00

2330.00

- +
100mg

￥4912.00

3930.00

- +

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Background

MS21570 is a selective GPR171 antagonist, with an IC50 of 220 nM.

MS21570 significantly attenuates this CNO-mediated increase in food intake. Interestingly, MS21570 causes a significant increase in center time compared to vehicle suggesting an effect on the anxiety-like behavior. Intra-BLA administration of MS21570 leads to an increase in open arm time on the elevated plus maze although there is no effect on locomotor activity during this test. Interestingly, when administered before and immediately following fear conditioning, MS21570 significantly attenuates freezing measured 24 hours later. Behavioral differences between systemic and intra-BLA administration of MS21570 could be due to the pharmacokinetic and pharmacodynamic properties of the drug. Further studies are needed to characterize the GPR171 antagonist[1].

[1]. Bobeck EN, et al. The BigLEN-GPR171 Peptide Receptor System Within the Basolateral Amygdala Regulates Anxiety-Like Behavior and Contextual Fear Conditioning. Neuropsychopharmacology. 2017 Dec;42(13):2527-2536.

Protocol

Animal experiment:

Mice[1]Male C57bl/6J or AgRP-IRES-Cre mice are 8-12 weeks old at the beginning of the experiment. Mice are habituated to the testing room 1 h prior to each experiment. Behaviors are videotaped and analyzed. Mice are injected with MS21570 (MS0021570_1: 5 mg/kg, i.p.) 15 min prior to elevated plus maze, open field, forced swim and contextual fear conditioning. For microinjection studies, MS21570 is injected 10 min prior testing and immediately following the contextual fear conditioning. Singly housed AgRP-IRES-Cre mice with cre-inducible DREADD in the arcuate nucleus receive MS21570 (3.5 mg/kg, i.p.) or vehicle (6% DMSO in saline) 15 min prior to CNO (1 mg/kg, i.p.) or saline injection. Food intake is measured at 1, 2, 4, and 8 hours post-injection[1].

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