Home Neuronal Signaling Dopamine Receptor antagonist Quetiapine (ICI-204636) fumarate For research use only.

Quetiapine (ICI-204636) fumarate

Synonyms: ICI-204636 fumarate

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.

Quetiapine (ICI-204636) fumarate Chemical Structure

Quetiapine (ICI-204636) fumarate Chemical Structure

CAS No. 111974-72-2

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Quetiapine (ICI-204636) fumarate Related Products

Signaling Pathway

Dopamine Receptor Signaling Pathways

Dopamine Receptor Signaling Pathway

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
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
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]
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

Chemical Information & Solubility

Molecular Weight 883.09 Formula

C46H54N6O8S2
CAS No. 111974-72-2 SDF Download Quetiapine (ICI-204636) fumarate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 36 mg/mL ( (40.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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.

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