Antipsychotics |
Olanzapine also known as olanzapine, olanzapine Oran, is a common antipsychotic drugs, clinically used to control schizophrenia, bipolar mania and agitation symptoms of dementia, it can significantly improve schizophrenia negative (for example: apathy, emotional and social withdrawal, poverty of speech), positive symptoms (such as: delusions, hallucinations, thought disorder, hostility and suspicion), and it may also relieve common secondary schizophrenia and related disorders affective symptoms.
Good oral absorption, it needs 5-8 hours to reach the peak plasma concentration, and it is not affected by eating, it is metabolized in the liver through a combination of oxidation ; the major circulating metabolite is the 10-N-glucuronide.
Animal experiments show that olanzapine displays affinity on multiple receptors 5-HT, dopamine D, α-adrenergic, histamine H et , the affinity with 5-HT2 receptor in vitro and in vivo is greater than its affinity for dopamine D2 receptors.
Animal behavior studies show that olanzapine has a 5-HT, dopamine, and cholinergic antagonism effect, and it is consistent with its receptor binding situation.
Electrophysiological studies show that olanzapine selectively reduces the limbic system (A10) dopaminergic neurons discharge, while the effect on the striatal (A9) motor path function is very small. In the reaction below to produce froze dosage levels, it can reduce the conditioned avoidance response. Different with other antipsychotics, olanzapine increases the anxiolytic response in test .
The above information is edited by the chemicalbook of Tian Ye. |
Chemical properties |
Crystallization from acetonitrile, melting point of 195 ℃. |
Uses |
Used to control schizophrenia, bipolar mania and other diseases |
Production method |
4-amino-2-methyl-10H-thieno [2,3-b] [1,5] benzo-diazepin-hydrochloride and N-methylpiperazine in toluene and dimethylsulfoxide , reflux under nitrogen for 20h, to obtain olanzapine. |
Chemical Properties |
Yellow Crystalline Powder |
Uses |
A serotonin (5-HT2) and dopamine (D1/D2) receptor antagonist with anticholinergic activity. Antipsychotic. |
Uses |
intermediate for Imidacloprid, Indobufen, Nitroguanidine, Nalorphine, Tazarotene, Trovafloxacin |
Uses |
anti-ulcer, gastrointestinal-emptying agent enhances motility in the upper gastrointestinal tract |
Definition |
ChEBI: A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. |