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Quetiapine (ICI-204636) fumarate Dopamine Receptor Antagonista

Name: Quetiapine (ICI-204636) fumarate
Brand: Selleck Chemicals
SKU: S1763
Rating: 5 (6 reviews)

Cat. No.: S1763

Quetiapine Fumarate (ICI-204636) es un antipsicótico atípico utilizado en el tratamiento de la esquizofrenia, la manía bipolar I, la depresión bipolar II, la depresión bipolar I y muestra afinidad por varios receptores de neurotransmisores, incluyendo los receptores de serotonina, dopamina, histamina y adrenérgicos.

Quetiapine (ICI-204636) fumarate Dopamine Receptor Antagonista Chemical Structure

Estructura química

Peso molecular: 883.09

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Control de calidad (Quality Control)

Lote: Pureza: 99.98%

99.98

Dianas relacionadas	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Otros Dopamine Receptor Inhibidores	MPTP Hydrochloride Trifluoperazine Trifluoperazine 2HCl Penfluridol Rotundine Domperidone Sulpiride Azaperone Levosulpiride SCH-23390 hydrochloride

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	883.09	Fórmula	C₄₆H₅₄N₆O₈S₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	111974-72-2	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	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

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 36 mg/mL (40.76 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (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.
Referencias	[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/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2026-05-26)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT07152184	NOT_YET_RECRUITING	Patient With Schizophrenia Spectrum Disorder; NLM Classification WM 203, Psychology:Schizophrenic Psychology; Schizophrenia Spectrum and Other Psychotic Disorders	University Hospital, Strasbourg, France	2026-10-01	PHASE2
NCT06433635	ACTIVE_NOT_RECRUITING	Bipolar I Disorder; Depression	Massachusetts General Hospital	2024-10-01	PHASE4
NCT05085808	WITHDRAWN	Delirium; Morality; Quality of Life; Psych; Treatment Side Effects	University of Southern California	2028-03-01	PHASE4
NCT07654348	NOT_YET_RECRUITING	Bipolar Disorder II	First Affiliated Hospital of Zhejiang University	2026-07-01	PHASE2
NCT06062953	RECRUITING	Psychiatric Disorders; Insomnia	Lone Baandrup	2023-09-18	PHASE2; PHASE3
NCT07760168	NOT_YET_RECRUITING	Treatment Resistant Depression (TRD)	All India Institute of Medical Sciences, Bhubaneswar	2026-08-30	PHASE3

Preguntas frecuentes (Frequently Asked Questions)

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

Respuesta:
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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