Norquetiapine
Based on 1 publication(s) in Google Scholar
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.
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- Purity: 99.89%
- CAS No.: 5747-48-8
- 화학식: C17H17N3S
- 분자량:295.41
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보관:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Norquetiapine
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT1A Receptor |
5-HT2C Receptor |
5-HT7 Receptor |
Norquetiapine (5 μM) blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner [1].
Norquetiapine (10-30 μM, 7.5-30 min) selectively inhibits HCN1 currents in Xenopus laevis oocytes by shifting the voltage-dependence of activation to more hyperpolarized potentials and slowing channel opening, with an IC50 of 13.9 μM[2].
Norquetiapine (30 μM, 7.5-15 min) inhibits HCN4 channels in Xenopus laevis oocytes with reduced efficacy compared to HCN1 and has no significant effect on HCN2 channels[2].
Norquetiapine (30 μM, 7.5 min) inhibits HCN1 channels primarily from the closed state in Xenopus laevis oocytes, with minimal effect on open-state channels[2].
Norquetiapine exhibits varying affinities for multiple receptors and the norepinephrine transporter (NET) with Ki values as follows: 196 nM for D2, 48 nM for 5-HT2A, 107 nM for 5-HT2C, 45 nM for 5-HT1A, 76 nM for 5-HT7, 3.5 nM for H1, 144 nM for Alpha-1, 237 nM for Alpha-2, and 58 nM for NET[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Norquetiapine (0.1-1.0 mg/kg, i.p., daily, 12-14 days) displays potent antidepressant-like activity in VMAT2 heterozygous mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (2 months old) were injected with LPS(1 mg/kg)[3]
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Dosage:10 mg/kg
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Administration:i.p. once daily for 14 days
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Result:Increased serum IL-10 levels and decreased serum IFN-γ levels at 4 h post-LPS challenge.
Showed similar regulatory effects on hippocampal IL-10 and IFN-γ gene expression at 4 h post-LPS.
Led to increased IL-1β expression in the PFC at 4 h post-LPS.
Attenuated the increased Il-10 in different brain regions at 24 h post-LPS.
Had no significant effect on LPS-induced changes in anhedonia and short-term recognition memory.
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Animal Model:C57BL6 VMAT2 mice (with transmembrane 3 and 4 regions deleted)[5]
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Dosage:0.1, 0.5, 1.0 mg/kg
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Administration:i.p. daily for 12 or 14 days
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Result:Reduced immobility time in VMAT2 heterozygous mice in the tail suspension test at doses as low as 0.1 mg/kg after acute administration.
Decreased immobility time in VMAT2 heterozygous mice in the tail suspension test following 14-day administration of 0.5 mg/kg.
Showed no significant effect on locomotor activity in both wild-type and VMAT2 heterozygous mice in open-field tests after acute or 14-day administration.
Chemical Information
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CAS No. 5747-48-8
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Appearance Solid
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분자량 295.41
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화학식 C17H17N3S
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Color White to yellow
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SMILES
C12=CC=CC=C1N=C(C3=CC=CC=C3S2)N4CCNCC4
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Synonyms
N-Desalkylquetiapine
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Metab Dispos
2025 Nov;53(11):100169. PMID: 41100927
용액&용해도
DMSO : 100 mg/mL (338.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (289 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3851 mL | 16.9256 mL | 33.8511 mL | 84.6279 mL |
| 5 mM | 0.6770 mL | 3.3851 mL | 6.7702 mL | 16.9256 mL | |
| 10 mM | 0.3385 mL | 1.6926 mL | 3.3851 mL | 8.4628 mL | |
| 15 mM | 0.2257 mL | 1.1284 mL | 2.2567 mL | 5.6419 mL | |
| 20 mM | 0.1693 mL | 0.8463 mL | 1.6926 mL | 4.2314 mL | |
| 25 mM | 0.1354 mL | 0.6770 mL | 1.3540 mL | 3.3851 mL | |
| 30 mM | 0.1128 mL | 0.5642 mL | 1.1284 mL | 2.8209 mL | |
| 40 mM | 0.0846 mL | 0.4231 mL | 0.8463 mL | 2.1157 mL | |
| 50 mM | 0.0677 mL | 0.3385 mL | 0.6770 mL | 1.6926 mL | |
| 60 mM | 0.0564 mL | 0.2821 mL | 0.5642 mL | 1.4105 mL | |
| 80 mM | 0.0423 mL | 0.2116 mL | 0.4231 mL | 1.0578 mL | |
| 100 mM | 0.0339 mL | 0.1693 mL | 0.3385 mL | 0.8463 mL |
Norquetiapine Related Classifications
HY-W052508 Related Classifications
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