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DR4485 hydrochloride

Names

[ CAS No. ]:
402942-53-4

[ Name ]:
DR4485 hydrochloride

[Synonym ]:
6-Chloro-2a-{4-[4-(4-chlorophenyl)-3,6-dihydro-1(2H)-pyridinyl]butyl}-2a,3,4,5-tetrahydrobenzo[cd]indol-2(1H)-one hydrochloride (1:1)
Benz[cd]indol-2(1H)-one, 6-chloro-2a-[4-[4-(4-chlorophenyl)-3,6-dihydro-1(2H)-pyridinyl]butyl]-2a,3,4,5-tetrahydro-, hydrochloride (1:1)

Biological Activity

[Description]:

DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14)[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT7 Receptor:8.14 (pKi)


[In Vitro]

DR4485 (MZ54 WT cells; 6 µM or 8 µM) hydrochloride induces autophagy as well as cell death that is diminished by KO of ATG5 and ATG7[2].

[References]

[1]. Kikuchi C, et al. New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. Bioorg Med Chem Lett. 2003;13(1):61-64.

[2]. Meyer N, et al. Autophagy activation, lipotoxicity and lysosomal membrane permeabilization synergize to promote pimozide- and loperamide-induced glioma cell death [published online ahead of print, 2021 Jan 19]. Autophagy. 2021;1-20.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H29Cl3N2O

[ Molecular Weight ]:
491.880

[ Exact Mass ]:
490.134552

Related Compounds