DR 4485 hydrochloride
Chemical Name: 6-Chloro-2a-[4-[4-(4-chlorophenyl)-3,6-dihydro-1(2H)-pyridinyl]butyl]-2a,3,4,5-tetrahydrobenz[cd]indol-2(1H)-one hydrochloride
Purity: ≥98%
Biological Activity
DR 4485 hydrochloride is a high affinity and selective 5-HT7 antagonist (pKi = 8.14). Exhibits selectivity for 5-HT7 over other 5-HT receptors. Inhibits 5-HT-induced cAMP accumulation in HEK-293 cells expressing the 5-HT7 receptor. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors
PLoS Pathog, 2016;12(5):e1005651. -
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.
Kikuchi et al.
Bioorg.Med.Chem.Lett., 2003;13:61 -
Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.
Medina et al.
J.Med.Chem., 2009;52:2384
Product Datasheets
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Citations for DR 4485 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for DR 4485 hydrochloride include:
3 Citations: Showing 1 - 3
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Autophagy activation, lipotoxicity and lysosomal membrane permeabilization synergize to promote pimozide- and loperamide-induced glioma cell death.
Authors: Gerd Et al.
Autophagy 2021;17:3424-3443
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Neuromodulator Signaling Bidirectionally Controls Vesicle Numbers in Human Synapses.
Authors: Thomas C Et al.
Cell 2019;179:498-513.e22
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A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors.
Authors: Chan Et al.
PLoS Pathog 2016;12:e1005651
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