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Lurasidone (SM13496; SM-13496; Latuda) is an atypical antipsychotic drug approved for the treatment of schizophrenia and bipolar disorders. It effectively inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A, and noradrenaline α2C with IC50 values of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM, and 10.8 nM, respectively.
| Targets |
5-HT2A ( Ki = 0.5 nM ); 5-HT7 receptor ( Ki = 0.5 nM ); D2 receptor ( Ki = 1 nM ); 5-HT1A receptor ( Ki = 6.4 nM )
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| ln Vitro |
Lurasidone (SM-13496) exhibits an antagonistic effect on dopamine D2 and 5-HT7, with IC50 values of 1.68±0.09 and 0.495±0.090 nM, respectively. Additionally, luerazidone (SM-13496) has an IC50 of 6.75±0.97 nM, making it a partial agonist of the 5-HT1A receptor. Lurasidone (SM-13496) exhibits a higher affinity for dopamine D2 and 5-HT2A receptors than other tested antipsychotics, according to in vitro receptor binding experiments. Lurasidone (SM-13496) has a KB value of 2.8±1.1 nM[1], which indicates that it opposes dopamine-stimulated [35S]GTPηS binding in a concentration-dependent manner. However, it does not increase [35S]GTPηS binding to the membrane preparations for dopamine D2 receptors on its own.
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| ln Vivo |
In the frontal cortex and striatum, luerazidone (SM-13496) dose-dependently raises the ratio of DOPAC/dopamine; however, it preferentially affects the frontal cortex over the striatum, particularly at higher doses. Comparable in potency to olanzapine (ED50 values 1.1 to 5.1 mg/kg), clozapine (ED50 values 9.5 to 290 mg/kg), and haloperidol (ED50 values 0.44 to 1.7 mg/kg), lurasidone (SM-13496) (ED50 values 2.3 to 5.0 mg/kg) exhibits a slightly lower potency. The ED50 values of lueradone (SM-13496) are 6.3 mg/kg, and it inhibits the conditioned avoidance response (CAR) in rats in a dose-dependent manner at 1 to 10 mg/kg. Lurasidone (SM-13496), with ED50 values of 5.6 and 3.0 mg/kg, respectively, dose-dependently inhibits p-chloroamphetamine (p-CAMP)-induced hyperthermia and tryptamine (TRY)-induced forepaw clonic seizures. Rats receive more shocks in the conflict test when given luerasidone (SM-13496) at doses ranging from 0.3 to 30 mg/kg (p<0.01), which is dose-dependent and statistically significant[1].
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| Animal Protocol |
Methamphetamine (MAP) (1 mg/kg i.p.) is injected into each individual SD rat in a clear plastic cage one hour after the drugs or vehicle are administered. Lurasidone (SM-13496) is given 1, 2, 4, and 8 hours prior to the MAP injection in order to test the effect's persistence. Following a 10-minute MAP injection, locomotor activity is monitored for 80 minutes. The ED50 value, which inhibits MAP-induced hyperactivity by 50% of the animals tested, is determined using four or five groups of six to thirteen rats[1].
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| References |
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| Molecular Formula |
C28H36N4O2S
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|---|---|
| Molecular Weight |
492.682
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| Exact Mass |
492.26
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| Elemental Analysis |
C, 68.26; H, 7.37; N, 11.37; O, 6.49; S, 6.51
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| CAS # |
367514-87-2
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| Related CAS # |
Lurasidone Hydrochloride; 367514-88-3; Lurasidone metabolite 14326 hydrochloride; Lurasidone-d8; 1132654-54-6; Lurasidone-d8 hydrochloride; Lurasidone metabolite 14326; 186204-33-1
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| Appearance |
White to off-white solid powder
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| SMILES |
C1CC[C@H]([C@@H](C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)[C@H]6[C@@H]7CC[C@@H](C7)[C@H]6C5=O
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| InChi Key |
PQXKDMSYBGKCJA-CVTJIBDQSA-N
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| InChi Code |
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
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| Chemical Name |
(1S,2R,6S,7R)-4-[[(1R,2R)-2-[[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl]cyclohexyl]methyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dione
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| Synonyms |
trade name Latuda; SM 13496; SM-13496; SM13496
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 7~20.83 mg/mL (14.2~42.3
mM)
Ethanol: ~3.3 mg/mL (~6.8 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0297 mL | 10.1486 mL | 20.2972 mL | |
| 5 mM | 0.4059 mL | 2.0297 mL | 4.0594 mL | |
| 10 mM | 0.2030 mL | 1.0149 mL | 2.0297 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05213143 | Active Recruiting |
Drug: Lurasidone | Schizophrenia | Sumitomo Pharma (Suzhou) Co., Ltd. | December 30, 2021 | Phase 4 |
| NCT03395392 | Active Recruiting |
Drug: NRX-101 Drug: Lurasidone HCl |
Bipolar Depression Suicidal Ideation and Behavior |
Second Affiliated Hospital of Guangzhou Medical University |
May 12, 2022 | Phase 2 Phase 3 |
| NCT03396068 | Active Recruiting |
Drug: Lurasidone HCl Drug: NRX-101 |
Bipolar Depression Suicidal Ideation |
NeuroRx, Inc. | December 1, 2019 | Phase 3 |
| NCT02731612 | Recruiting | Drug: lurasidone Drug: Placebo |
Bipolar Disorder | Nazlin Walji | May 8, 2017 | Phase 3 |
| NCT05351736 | Recruiting | Drug: Lurasidone | Schizophrenia | Fondazione IRCCS Ca' Granda, Ospedale Maggiore Policlinico |
January 26, 2022 | Phase 4 |
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