Norquetiapine

Norquetiapine (N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine 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 blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation[1][2][3][4][5].

Product Specifications

CAS Number

[5747-48-8]

Product Name Alternative

N-Desalkylquetiapine

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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

Type

Reference compound

Related Pathways

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

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/norquetiapine.html

Concentration

10mM

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H17N3S

Molecular Weight

295.41

Precautions

H302, H315, H319, H335

References & Citations

[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.