Antagonist of 5-HT2A and dopamine D2 receptors
CAS：132539-06-1
分子式：C17H20N4S
分子量：312.43
纯度：98%
存储：Store at -20°C

Background:

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

The 5-HT2 serotonin and D2 dopamine receptor s are subfamily of G protein-coupled receptors(GPCRs) [1].

In vitro: Binding studies showed that olanzapine interacted with keyreceptorsof interest in schizophrenia, exihibiting a nanomolar affinity for dopaminergic, serotonergic, alpha 1-adrenergic, and muscarinic receptors [1].

In vivo: Olanzapine was a potent antagonist at DAreceptorsand 5-HT receptors, but showed weaker activity at alpha-adrenergic and muscarinic receptors [1].Administration of Olanzapine at 0.5, 3 and 10 mg/kg (s.c.) increased the extracellulardopamine(DA) and norepinephrine (NE) levels in all three brain areas in a dose-dependent manner.The increases reached peaks 60-90 min after olanzapine administration and lasted for at least 2 h. The highest DA increases in the Acb and Cpu were induced by olanzapine at 3 mg/kg but at 10 mg/kg in the Pfc while the highest NE increase in the Pfc (414% ± 40) induced by 10 mg/kg olanzapine [2].In macaque monkeys, olanzapine treatment resulted in an 8-11% reduction in mean fresh brain weights as well as left cerebrum fresh weights and volumes [3].

参考文献:
[1]. Bymaster FP1,Rasmussen K,Calligaro DO,Nelson DL,DeLapp NW,Wong DT,Moore NA. In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug.J Clin Psychiatry.1997;58Suppl 10:28-36.
[2]. Li XM1,Perry KW,Wong DT,Bymaster FP. Olanzapine increases in vivodopamineand norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum.Psychopharmacology (Berl).1998 Mar;136(2):153-61.
[3]. Dorph-Petersen KA1,Pierri JN,Perel JM,Sun Z,Sampson AR,Lewis DA. The influence of chronic exposure to antipsychotic medications on brain size before and after tissue fixation: a comparison of haloperidol and olanzapine in macaque monkeys.Neuropsychopharmacology.2005 Sep;30(9):1649-61.