Olanzapine raw material Olanzapine Powder 132539-06-1

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Olanzapine Powder Usage and Synthesis.

Olanzapine is indicated for the acute and maintenance treatment of schizophrenia and other psychotic disorders with severe positive symptoms (e.g., delusions, hallucinations, thought disorders, hostility, and suspicion) and/or negative symptoms (e.g., affective apathy, emotional and social withdrawal, and impaired speech).

Olanzapine also relieves secondary affective symptoms common in schizophrenia and related disorders. For those who have achieved an initial benefit and need to continue treatment.

Uses and functions of Olanzapine.

For control of schizophrenia, bipolar mania and other disorders

Is a 5HT2-D2 antagonist. Used in the treatment of schizophrenia.

Pharmacological Effect of Olanzapine.

1. The mechanism of action of olanzapine, like that of other drugs used to treat schizophrenia, is unclear. The action of olanzapine in the treatment of schizophrenia may be through antagonism of dopamine and 5-hydroxytryptamine 2 (5-HT2).

The mechanism by which olanzapine treats acute manic episodes or mixed episodes associated with type I bipolar disorder is unknown.

2. Olanzapine has high affinity for the following receptors: 5 hydroxytryptamine 2A/2C (5HT2A/2C), 5 hydroxytryptamine 6 (5HT6) (Ki 4, 11, 5nM respectively), dopamine D1-4 (Ki 11-31nM), histamine H1 (Ki 7nM), adrenergic α1 receptor (Ki 19nM).

Olanzapine has a moderate affinity for 5 hydroxytryptamine 3 (5HT3) (Ki of 57nM), and muscarinic M1-5 (Ki of 73, 96, 132, 32, and 48nM, respectively). Olanzapine has a weak affinity for GABAA, BZD, and β-adrenergic receptors (Ki > 10 μM).

In addition to its antagonistic effects on dopamine and 5-HT2, olanzapine's affinity for other similar receptors could explain some of its other therapeutic effects and side effects.

The anticholinergic effects of olanzapine may be caused by its antagonism of muscarinic M1-5 receptors. The somnolent effect of olanzapine may be caused by its antihistamine H1 receptor action.

The hypotensive effect of olanzapine may be due to its anti-adrenergic alpha 1 receptor action.

Product Method of Bulk Olanzapine Powder.

4-Amino-2-methyl-10H-thieno[2,3-b][1,5]benzodiazepine hydrochloride and N-methylpiperazine in dimethylsulfoxide and toluene, refluxed for 20h under nitrogen protection to give olanzapine.

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