lurasidone

Modify Date: 2024-01-02 12:00:11

lurasidone structure	Common Name	lurasidone
	CAS Number	367514-87-2	Molecular Weight	492.676
	Density	1.3±0.1 g/cm3	Boiling Point	623.4±55.0 °C at 760 mmHg
	Molecular Formula	C₂₈H₃₆N₄O₂S	Melting Point	N/A
	MSDS	N/A	Flash Point	330.8±31.5 °C

Use of lurasidone

Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

Name	lurasidone
Synonym	More Synonyms

Description	Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
Target	IC50: 1.68 nM (dopamine D2), 0.495 nM (5-HT7), 6.75 nM (5-HT1A)[1]
In Vitro	Lurasidone is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone does not increase [35S]GTPγS binding to the membrane preparations for dopamine D2 receptors by itself, but it antagonizes dopamine-stimulated [35S]GTPγS binding in a concentration-dependent manner with a KB value of 2.8±1.1 nM[1].
In Vivo	Lurasidone 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 (ED50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values 0.44 to 1.7 mg/kg). Lurasidone (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED50 values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (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)[1].
Kinase Assay	[35S]GTPγS binding experiments for the human dopamine D2L or 5-HT1A receptors stably expressed in the membranes of recombinant Chinese hamster ovary (CHO) cells are performed. Shortly after dopamine (or serotonin) and/or Lurasidone are incubated for 20 min at room temperature with the cell membrane preparation containing [35S]GTPγS (0.05 nM for D2L or 0.2 nM for 5-HT1A), the membranes are filtered through glass filters and the radioactivity bound to each filter is measured with a liquid scintillation counter[1].
Animal Admin	SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kg i.p.) 1 h after the administration of drugs or vehicle. In the test of persistence of the effect, Lurasidone is administered 1, 2, 4, and 8 h before the MAP injection. Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 rats are used to calculate the ED50 value that inhibits MAP-induced hyperactivity by 50% of the animals tested[1].
References	[1]. Ishibashi T, et al. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81. [2]. Sakine Atila Karaca, et al. Development of a validated high-performance liquid chromatographic method for the determination of Lurasidone in pharmaceuticals. Marmara Pharm J. 2017;21 (4): 931-937.

Density	1.3±0.1 g/cm3
Boiling Point	623.4±55.0 °C at 760 mmHg
Molecular Formula	C₂₈H₃₆N₄O₂S
Molecular Weight	492.676
Flash Point	330.8±31.5 °C
Exact Mass	492.255890
PSA	84.99000
LogP	4.52
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.637

Hazard Codes	Xn

(1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-Benzothiazol-3-yl)-1-piperazinyl]methyl}cyclohexyl]methyl}-4-azatricyclo[5.2.1.0]decane-3,5-dione

lurasidone

4,7-Methano-1H-isoindole-1,3(2H)-dione, 2-[[(1R,2R)-2-[[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]methyl]cyclohexyl]methyl]hexahydro-, (3aR,4S,7R,7aS)-

DC Chemicals Limited
China
Product Name: lurasidone
Price: $450.0/100mg $800.0/250mg $1500.0/1g
Purity: 98.0%
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Zhejiang Hangyu API Co., Ltd
China
Product Name: lurasidone
Price: ￥Inquiry/1kg
Purity: 99.5%
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Henan Tianfu Chemical Co., Ltd.
China
Product Name: TIANFU-CHEM - lurasidone
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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