生物活性

• 描述Olanzapine is a D2 dopamine receptor antagonist with a high affinity for 5-HT2 serotonin. In vivo, sequential doses of olanzapine at 0.5, 3 and 10 mg/kg dose-dependently increased the extracellular dopamine (DA) and norepinephrine (NE) levels in all three brain areas. The increases appeared 30 min after olanzapine administration, reached peaks around 60 - 90 min and lasted for at least 2 h^[3]. The high dose of olanzapine (10 mg/kg ) increased the number of fos-like positive nuclei in mesolimbic areas connected to the extended amygdala^[4]. In vitro, olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01170117	Anorexia Nervosa	Not Applicable	Completed	-	United States, Maryland ... more >> Johns Hopkins Baltimore, Maryland, United States, 21287 United States, New York New York State Psychiatric Institute New York, New York, United States, 10032 Weill Cornell Medical Center White Plains, New York, United States, 10605 United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 Canada, Ontario Centre for Addiction and Mental Health Toronto, Ontario, Canada, M5T1R8 Collapse <<
  NCT00402324	Bipolar I Disorder	Phase 4	Completed	-	United States, Florida ... more >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Hialeah, Florida, United States, 33016 Collapse <<
  NCT00510211	-	-	Completed	-	France ... more >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Paris, France, 75674 Germany For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Bad Homburg, Germany, D-61350 Greece For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Thessaloniki, Greece, 54630 Collapse <<

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• 参考文献

• [1] Cipriani A, Rendell JM, et al. Olanzapine in long-term treatment for bipolar disorder. Cochrane Database Syst Rev. 2009 Jan 21;(1):CD004367.

  [2] Bymaster FP, Rasmussen K, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

  [3] Li XM, Perry KW, Wong DT, Bymaster FP. Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum. Psychopharmacology (Berl). 1998;136(2):153-161.

  [5] Bymaster FP, Rasmussen K, Calligaro DO, et al. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug. J Clin Psychiatry. 1997;58 Suppl 10:28-36.

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