Olanzapine (Synonyms: LY170053) |
| رقم الكتالوجGC12495 |
Olanzapine (LY170053) هو مضاد أحادي الأمين انتقائي نشط عن طريق الفم مع ارتباط تقارب عالي بالسيروتونين H1 ، 5HT2A / 2C ، 5HT3 ، 5HT6 (Ki = 7 ، 4 ، 11 ، 57 ، و 5 نانومتر ، على التوالي) ، الدوبامين D1-4 ( Ki = 11 إلى 31 نانومتر) ، المسكارين M1-5 (Ki = 1.9-25 نانومتر) ، والأدرينرجيك α ؛ مستقبل واحد (Ki = 19 نانومتر).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 132539-06-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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].
References:
[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.
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *