111974-74-4
Chemical Structure
Norquetiapine dihydrochloride
Synonym(s): N-Desalkylquetiapine dihydrochloride
- CAS No.: 111974-74-4
- Formula:C17H19Cl2N3S
- Molecular Weight:368.32
IUPAC Name: 11-(piperazin-1-yl)dibenzo[b,f][1,4]thiazepine dihydrochloride
InChIKey: PZQCQHZDUIIKFU-UHFFFAOYSA-N
SMILES: C12=CC=CC=C1N=C(C3=CC=CC=C3S2)N4CCNCC4.Cl.Cl
Biological Activity: Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation[1][2][3][4][5].
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Norquetiapine dihydrochloride | 99.91% | Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation. | ||||||||||||||||||||
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Norquetiapine dihydrochloride (Standard) | ≥98% | 11-(1-Piperazinyl)-dibenzo[b,f][1,4]thiazepine dihydrochloride (Standard) is the analytical standard of 11-(1-Piperazinyl)-dibenzo[b,f][1,4]thiazepine dihydrochloride. This product is intended for research and analytical applications. | ||||||||||||||||||||
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- [1]. Kim DH, Park KS, Park SH, Hahn SJ, Choi JS. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Eur J Pharmacol. 2020 Oct 15;885:173532. [Content Brief]
- [2]. Jean Jacques A, et al. Inhibition of HCN1 currents by norquetiapine, an active metabolite of the atypical anti-psychotic drug quetiapine. Front Pharmacol. 2024 Oct 7;15:1445509. [Content Brief]
- [3]. Jaehne EJ, et al. The effect of the antipsychotic drug quetiapine and its metabolite norquetiapine on acute inflammation, memory and anhedonia. Pharmacol Biochem Behav. 2015 Aug;135:136-44. [Content Brief]
- [4]. López-Muñoz F, et al. Active metabolites as antidepressant drugs: the role of norquetiapine in the mechanism of action of quetiapine in the treatment of mood disorders. Front Psychiatry. 2013 Sep 12;4:102. [Content Brief]
- [5]. Jensen NH, et al. N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity. Neuropsychopharmacology. 2008 Sep;33(10):2303-12. [Content Brief]
