Quetiapine (ICI-204636) fumarate

For research use only.

Catalog No.S1763

3 publications

Quetiapine (ICI-204636) fumarate Chemical Structure

CAS No. 111974-72-2

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.

Selleck's Quetiapine (ICI-204636) fumarate has been cited by 3 publications

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Biological Activity

Description 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.
Targets
Dopamine receptor [1] Histamine receptor [1] Adrenergic Receptor [1]
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. [1]

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. [1] 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. [2] 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. [3] 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. [4]

Protocol

Solubility (25°C)

In vitro DMSO 36 mg/mL (40.76 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 883.09
Formula

C46H54N6O8S2

CAS No. 111974-72-2
Storage powder
in solvent
Synonyms N/A
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00837343 Unknown status Drug: quetiapine fumarate tablet (Seroquel) 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 Drug: Quetiapine fumarate|Drug: Haloperidol Acute Schizophrenia Sichuan University August 2008 Phase 4
NCT00631722 Completed Drug: Quatiapine Fumarate|Drug: Haloperidol Schizophrenia Peking University May 2007 Not Applicable
NCT00448578 Completed Drug: Quetiapine Fumarate|Drug: Lithium Mania|Bipolar Disorder AstraZeneca August 2005 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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:

    S1763 Quetiapine Fumarate can be dissolved in 0.5% CMC Na at 30 mg/ml as a suspension. It is fine for oral gavage.

Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID