Olanzapine

Catalog No.S2493 Synonyms: LY170053

For research use only.

Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Olanzapine Chemical Structure

CAS No. 132539-06-1

Selleck's Olanzapine has been cited by 13 publications

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Biological Activity

Description Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Targets
5-HT2 [1] D2 receptor [1]
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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 312.43975
Formula

C17H20N4S

CAS No. 132539-06-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC2=C(S1)NC3=CC=CC=C3N=C2N4CCN(CC4)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04075955 Completed Drug: Zyprexa® (OLANZapine 5MG)|Drug: Emend® (Aprepitant) Chemotherapy-induced Nausea and Vomiting CR-CSSS Champlain-Charles-Le Moyne April 29 2019 Phase 3
NCT03118986 Recruiting Drug: Olanzapine|Drug: Placebo Oral Tablet Vomiting in Infants and/or Children|Nausea|Hematopoietic System--Cancer The Hospital for Sick Children|University of California San Francisco|Children''s Mercy Hospital Kansas City|St. Justine''s Hospital|Columbia University|Medical University of South Carolina August 10 2017 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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