product name Olanzapine
Description: Olanzapine (also known as LY170053) is an atypical antipsychotic with high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. It is a dopamine antagonist and is classified as a thienobenzodiazepine. Binding studies showed that olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors. It is approved by the U.S. FDA for the treatment of schizophrenia and bipolar disorder. Olanzapine is structurally similar to clozapine and quetiapine.
References: J Clin Psychiatry. 1997;58 Suppl 10:28-36; Neuropsychopharmacology. 2000 Sep;23(3):250-62.
312.44
Formula
C17H20N4S
CAS No.
132539-06-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 63 mg/mL (201.6 mM)
Water: <1 mg/mL
Ethanol: 9 mg/mL (28.8 mM)
Solubility (In vivo)
Synonyms
LY170053
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413889
| In Vitro |
In vitro activity: 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). Kinase Assay: Cell Assay: |
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| 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. 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. 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. Olanzapine results in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes in macaque monkeys. 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. |
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| References | J Clin Psychiatry. 1997;58 Suppl 10:28-36; Neuropsychopharmacology. 2000 Sep;23(3):250-62. |
