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Lurasidone(CAS#367514-87-2)

Chemical Property:

Molecular Formula C28H36N4O2S
Molar Mass 492.68
Density 1.273
Melting Point 146-149°C
Boling Point 623.4±55.0 °C(Predicted)
Flash Point 330.8°C
Solubility Chloroform (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Heated)
Vapor Presure 1.85E-15mmHg at 25°C
Appearance Powder
Color White to Off-White
pKa 8.41±0.50(Predicted)
Storage Condition -20°C Freezer
Refractive Index 1.636
In vitro study Lurasidone (SM-13496) is an antagonist of dopamine D 2 and 5-HT 7 with IC 50 s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT 1A receptor with an IC 50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D 2 and 5-HT 2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) does not increase [ 35 S]GTPγS binding to the membrane preparations for dopamine D 2 receptors by itself, but it antagonizes dopamine-stimulated [ 35 S]GTPγS binding in a concentration-dependent manner with a K B value of 2.8±1.1 nM.
In vivo study Lurasidone (SM-13496) dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (SM-13496) (ED 50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED 50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED 50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED 50 values 0.44 to 1.7 mg/kg). Lurasidone (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED 50 values are 6.3 mg/kg. Lurasidone (SM-13496) dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED 50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (SM-13496) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01).

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Introduction

Lysergic acid diethylamide (LSD) is a potent hallucinogen, also known as a psychedelic drug. It is obtained from lysergic acid through a series of chemical synthesis. Lurasidone is a colorless and odorless crystal that is usually found in the form of pieces of paper or small biscuits.It can produce a series of perceptual and cognitive changes after taking it, including visual, auditory and emotional changes, causing people to hallucinate and auditory hallucinations. Lurasidone is widely used in fields such as psychological research, neuroscience research, and mind exploration.The preparation method of lurasidone is mainly obtained by chemical synthesis of lysergic acid. Specifically, lysergic acid is first reacted with acetic anhydride to obtain acetylergic anhydride, and then by reacting with ethanol, ethyl acetyl lysergic acid is obtained. By hydrolysis or acid hydrolysis, lurasidone is obtained.


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