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Olanzapine

Name: Olanzapine
Brand: Selleck Chemicals
SKU: S2493
Rating: 5 (13 reviews)

Synonyms: LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera

Catalog No.S2493 Purity: 99.99%

Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Olanzapine Chemical Structure

CAS: 132539-06-1

Selleck's Olanzapine has been cited by 13 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Biological Activity

Description

Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Targets

5-HT2 ^[1]

D2 receptor ^[1]

In vitro
In vitro	Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. Olanzapine has a receptor profile that is similar to that of clozapine: it is relatively nonselective at dopamine receptor subtypes and it shows selectivity for mesolimbic and mesocortical over striatal dopamine tracts (electrophysiology; Fos). ^[1]

In Vivo
In vivo	Olanzapine is a potent antagonist at DA receptors (DOPAC levels; pergolide-stimulated increases in plasma corticosterone) and 5-HT receptors (quipazine-stimulated increases in corticosterone), but is weaker at alpha-adrenergic and muscarinic receptors. ^[1] Olanzapine combined with fluoxetine produces robust, sustained increases of extracellular levels of dopamine ([DA](ex)) and norepinephrine ([NE](ex)) up to 361% and 272% of the baseline in rat prefrontal cortex, respectively, which are significantly greater than either drug alone. ^[2] Olanzapine at 0.5 mg/kg, 3 mg/kg and 10 mg/kg (s.c.) dose-dependently increases the extracellular dopamine (DA) and norepinephrine (NE) levels in rat prefrontal cortex, nucleus accumbens and striatum. Olanzapine also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. ^[3] Olanzapine results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. ^[4] Olanzapine results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. Olanzapine results in marked hepatic insulin resistance. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06107803	Recruiting	Negative Symptoms in Schizophrenia	Minerva Neurosciences	October 13 2023	Phase 1
NCT05977855	Recruiting	Behavioral and Psychiatric Symptoms of Dementia	Fondazione IRCCS San Gerardo dei Tintori	July 1 2023	Not Applicable
NCT05462340	Recruiting	Schizophrenia	Washington University School of Medicine	August 18 2022	Phase 1

References

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Chemical lnformation & Solubility

Molecular Weight	312.43975	Formula	C₁₇H₂₀N₄S
CAS No.	132539-06-1	SDF	Download Olanzapine SDF
Smiles	CC1=CC2=C(S1)NC3=CC=CC=C3N=C2N4CCN(CC4)C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 62 mg/mL ( (198.43 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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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Handling Instructions

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