lurasidone Chemical Properties

Melting point:

146-149°C

Boiling point:

623.4±55.0 °C(Predicted)

Density 

1.273

storage temp. 

-20°C Freezer

solubility 

Chloroform (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Heated)

pka

8.41±0.50(Predicted)

form 

Solid

color 

White to Off-White

InChI

InChI=1S/C28H36N4O2S/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2/t18-,19+,20-,21-,24+,25-/m0/s1

InChIKey

PQXKDMSYBGKCJA-CVTJIBDQSA-N

SMILES

C1(=O)[C@]2([H])[C@@]([H])([C@]3([H])C[C@@]2([H])CC3)C(=O)N1C[C@@H]1CCCC[C@H]1CN1CCN(C2C3=C(SN=2)C=CC=C3)CC1

CAS DataBase Reference

367514-87-2

Safety Information

Hazardous Substances Data

367514-87-2(Hazardous Substances Data)

lurasidone Usage And Synthesis

Drug for the treatment of schizophrenia

Lurasidone is developed by Japan's Dainippon Sumitomo Pharma which is an atypical antipsychotic,and is a classification of drug registration 3.1 class, it is suitable for the treatment of patients with schizophrenia. Its efficacy is Determined in four six weeks in adult patients with schizophrenia controlled studies. The exact mechanism of the treatment of schizophrenia, like other atypical antipsychotics ,is not very clear,and may be related to the antagonism of the dopamine D2 and serotonin 2A (5-HT2A) receptors. For the treatment of schizophrenia, a study has reported lurasidone can improve cognitive function.
October 28, 2010 ,the FDA approved lurasidone hydrochloride (lurasidone HCI) tablets once a day for the first-line treatment of patients with schizophrenia, the trade name is Latuda.
Dosage: The recommended starting dose is 40 mg/d, the effective dose range is 40~120 mg /· d, the maximum recommended dose is 80 mg /· d. It should be taken with food.
Adverse reaction: common adverse reactions are somnolence, akathisia, nausea, Parkinson's disease-like symptoms and emotional anxiety. Lurasidone has no physical dependence, less likely to cause weight gain, it does not cause glucose, lipids (lipids), it changs the period between ECG and QT.
The above information is edited by the Chemicalbook of Tian Ye.

Description

The atypical antipsychotic lurasidone (also known as SM-13496) was approved in the United States in 2010 as an oral agent for the treatment of patients with schizophrenia. Lurasidone has potent affinity for D₂ (K_i= 1.7 nM) and 5-HT_2A (K_i= 2.0 nM) receptors and acts as an antagonist at both receptors. It is also a partial agonist at the 5-HT_1A receptor and, unlike other atypical agents, is a potent antagonist at the 5-HT₇ receptor; both of these activities are thought to confer beneficial cognitive properties. Lurasidone is further differentiated by its lack of affinity for muscarinic and histamine H₁ receptors and its weak affinity for the 5-HT_2C receptor. Antagonism at H₁ and 5-HT_2C receptors has been implicated in weight gain associated with atypical agents, while muscarinic receptor antagonism is associated with cognitive deficits.

Originator

Dainippon Sumitomo Pharma (Japan)

Definition

ChEBI: An N-arylpiperazine that is (3aR,4S,7R,7aS)-2-{[(1R,2R)-2-(piperazin-1-ylmethyl)cyclohexyl]methyl}hexahydro-1H-4,7-m thanoisoindole-1,3(2H)-dione in which position N4 of the piperazine ring is substituted by a 1,2-benzothiazol-3-yl group. Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizoph enia.

brand name

Latuda

lurasidone(367514-87-2)Related Product Information

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