Norquetiapine (dihydrochloride)

Norquetiapine (N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine , 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].

111974-74-4

N-Desalkylquetiapine (dihydrochloride)

12352005

H302, H315, H319, H335

5-HT Receptor; Drug Metabolite; HCN Channel; Serotonin Transporter

GPCR/G Protein; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Neurological Disease

99.91

C12=CC=CC=C1N=C(C3=CC=CC=C3S2)N4CCNCC4.Cl.Cl

C17H19Cl2N3S

368.32

H302, H315, H319, H335

[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.|[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.|[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.|[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.|[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.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

http://file.medchemexpress.com/batch_PDF/HY-W040555/

Reference compound2

Phase 1