research use only
Cat.No.S2493
| Related Targets | Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR |
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| Other 5-HT Receptor Inhibitors | WAY-100635 Maleate Puerarin Serotonin (5-HT) HCl SB269970 HCl Ketanserin BRL-15572 Dihydrochloride Nuciferine RS-127445 Flopropione Azacyclonol |
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In vitro |
DMSO
: 62 mg/mL
(198.43 mM)
Ethanol : 15 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 312.43975 | Formula | C17H20N4S |
Storage (From the date of receipt) | |
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| CAS No. | 132539-06-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera | Smiles | CC1=CC2=C(S1)NC3=CC=CC=C3N=C2N4CCN(CC4)C | ||
| Targets/IC50/Ki |
5-HT2
D2 receptor
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| In vitro |
Olanzapine interacts with key receptors of interest in schizophrenia, having a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. This compound 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). |
| 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. This compound 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. It 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. This chemical also increases extracellular levels of a DA metabolite, DOPAC, and tissue concentrations of a released DA metabolite, 3-methoxytyramine. It results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. This agent results in substantial increases in adiposity: increased total body fat reflecting marked increases in subcutaneous and visceral adipose stores. It results in marked hepatic insulin resistance. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06288854 | Not yet recruiting | Weight Gain |
Rajavithi Hospital |
April 3 2024 | Not Applicable |
| NCT06319170 | Recruiting | Schizophrenia Schizoaffective Disorder |
Teva Branded Pharmaceutical Products R&D Inc. |
March 28 2024 | Phase 1 |
| NCT06315283 | Recruiting | Schizophrenia |
Teva Branded Pharmaceutical Products R&D Inc. |
March 20 2024 | Phase 1 |
| NCT06253546 | Recruiting | Schizophrenia |
Teva Branded Pharmaceutical Products R&D Inc. |
March 28 2024 | Phase 1 |
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