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Deschloroclozapine

CAS No. : 1977-07-7

MCE 站：Deschloroclozapine

产品活性：Deschloroclozapine 是有效的，高亲和力的，选择性的，代谢稳定的基于毒蕈碱的 DREADDs 的激动剂。Deschloroclozapine 抑制 [³H] 苄基喹啉基 (QNB) 与 hM₃Dq 和 hM₄Di 的结合，K_i 值分别为 6.3 和 4.2 nM。据报道 Deschloroclozapine 在小鼠和非人类灵长类动物中都有多种用途。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR

In Vitro: Deschloroclozapine has greater potencies for DREADDs than previous agonists in vitro. Deschloroclozapine is a potent agonist for hM₃Dq with an EC₅₀=0.13 nM. Deschloroclozapine is also a potent agonist for hM₄Di with an EC₅₀=0.081 nM.
Deschloroclozapine is a potent and selective agonist for hM₃Dq and hM₄Di, it does not display significant agonistic activity for any of the 318 tests wild-type GPCRs at <10 nM.

In Vivo: Deschloroclozapine (100 μg/kg; i.v.) exhibits good brain concentration profiles and biostability. Pharmacokinetic studies confirmed that Deschloroclozapine is rapidly accumulated in mouse brains and monkey CSF, while its metabolites are negligible.
Deschloroclozapine (1 μg/kg; i.p.) selectively and rapidly enhances neuronal activity via hM₃Dq-DREADD in vivo, Deschloroclozapine can also be utilized for in vivo neuronal silencing by activating hM₄Di, an inhibitory DREADD.
Deschloroclozapine (1-100 μg/kg; i.v.) selectively induces hM₃Dq-mediated metabolic activity.
Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM₄Di-expressing monkeys.

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