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JHU 37152 是一种有效的脑渗透性 DREADD 激动剂,在 HEK-293 细胞中对 hM3Dq 和 hM4Di DREADD 的 EC50 分别为 5?nM 和 0.5?nM。
High affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.8 nM and 8.7 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in vitro, respectively). Selectively displaces [3H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. Inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons. Brain penetrant in mice, rats and non-human primates.
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