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Quetiapine (ICI-204636) fumarate Dopamine Receptor antagonist

Name: Quetiapine (ICI-204636) fumarate
Brand: Selleck Chemicals
SKU: S1763
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S1763

Quetiapine Fumarate (ICI-204636) is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression and shows affinity for various neurotransmitter receptors including serotonin, dopamine, histamine, and adrenergic receptors.

Chemical Structure

Molecular Weight: 883.09

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Dopamine Receptor Inhibitors	MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol SCH-23390 hydrochloride Domperidone SKF38393 HCl Sulpiride Azaperone C-DIM12

Solubility

In vitro
Batch:

DMSO : 36 mg/mL (40.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	883.09	Formula	C₄₆H₅₄N₆O₈S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	111974-72-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ICI-204636 fumarate			Smiles	C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42.C1CN(CCN1CCOCCO)C2=NC3=CC=CC=C3SC4=CC=CC=C42.C(=CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	Dopamine receptor Histamine receptor Adrenergic Receptor
In vitro	Quetiapine shows affinity for various neurotransmitter receptors including serotonin, dopamine, histamine, and adrenergic receptors and has binding characteristics at the dopamine-2 receptor similar to those of clozapine.
In vivo	Quetiapine has a preclinical profile suggestive of antipsychotic activity with a reduced tendency to cause extrapyramidal symptoms (EPS) and sustained prolactin elevation. Guetiapine alters neurotensin neurotransmission and c-fos expression in limbic but not motor brain regions. Quetiapine also demonstrates clozapine-like activity in a range of behavioral and biochemical tests and may possess neuroprotective properties. Quetiapine dose-dependently prevents schizophrenia and depression in hippocampal cell proliferation and BDNF expression caused by chronic restraint stress (CRS) in rats. Guetiapine (5 mg/kg) combined with Venlafaxine (2.5 mg/kg) increases hippocampal cell proliferation and prevents BDNF decrease in stressed rats, whereas each of the drugs exerts mild or no effects. Guetiapine produces selective effects on cortical and limbic regions of the brain and in particular on dopaminergic neurotransmission in these regions. Guetiapine produces lower levels of putamenal DA D2r occupancy than those reported for typical APDs. Quetiapine also produces preferential occupancy of temporal cortical DA D2r, 46.9%, but does not spare occupancy of substantia nigra DA D2r. Guetiapine attenuates the decrease in levels of brain-derived neurotrophic factor (BDNF) in the hippocampi of rats subjected to chronic-restraint stress. Guetiapine (10 mg/kg) reverses the stress-induced suppression of hippocampal neurogenesis, evidenced in the numbers of BrdU-labeled and pCREB-positive cells that are comparable to those in non-stressed rats but higher than those in the vehicle-treated rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12562141/ [2] https://pubmed.ncbi.nlm.nih.gov/16652337/ [3] http://www.ncbi.nlm.nih.gov/pubmed/ 16738543 [4] https://pubmed.ncbi.nlm.nih.gov/16271709/ [5] https://pubmed.ncbi.nlm.nih.gov/8369191/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00837343	Unknown status	Bipolar Disorder	Guangzhou Mental Hospital\|First Affiliated Hospital of Jinan University\|Second Affiliated Hospital of Guangzhou Medical University\|Guangzhou mental Hospital Attached to Guangzhou Civil Affairs Bureau	December 2008	Phase 4
NCT00838032	Unknown status	Acute Schizophrenia	Sichuan University	August 2008	Phase 4
NCT00631722	Completed	Schizophrenia	Peking University	May 2007	Not Applicable
NCT00448578	Completed	Mania\|Bipolar Disorder	AstraZeneca	August 2005	Phase 3

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Handling Instructions

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Frequently Asked Questions

Question 1:
I want to know if your recommended formulation for in vivo experiments on the website is suitable for oral administration or injection?

Answer:
It can be dissolved in 0.5% CMC Na at 30 mg/ml as a suspension and is fine for oral gavage.

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