lurasidone

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

CAS No. 367514-87-2

サイズ	価格(税別)	在庫状況
25mg	JPY 15900	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（2）

製品安全説明書

現在のバッチを見る： S571401 DMSO] 7 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度： 99.96%

99.96

lurasidone関連製品

関連ターゲット	D1 receptor D2 receptor D3 receptor D5 receptor DAT D4 receptor	もっと見る
関連製品	Chlorpromazine Chlorpromazine HCl MPTP hydrochloride Trifluoperazine Trifluoperazine 2HCl Dopamine HCl Prochlorperazine dimaleate salt Quetiapine (ICI-204636) fumarate Fluphenazine dihydrochloride Penfluridol Haloperidol SCH-23390 hydrochloride Metoclopramide HCl Amantadine HCl Pramipexole Domperidone Amisulpride Paliperidone Levodopa SKF38393 HCl Metoclopramide hydrochloride hydrate Sulpiride Droperidol Azaperone C-DIM12 ONC206 Pimozide Pramipexole 2HCl Monohydrate Rotigotine Levosulpiride Chlorprothixene Metoclopramide Tetrahydropalmatine 6-OHDA (Oxidopamine hydrobromide) Fenoldopam mesylate Triflupromazine hydrochloride Rotundine Piribedil Tetrabenazine (Xenazine) PD128907 HCl Lurasidone HCl Cabergoline Paliperidone Palmitate Benztropine mesylate Tiapride Hydrochloride Ropinirole HCl	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

Dopamine Receptorシグナル伝達経路

Dopamine Receptor阻害剤の選択性比較

生物活性

製品説明

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

Targets

5-HT2A ^[1] (Cell-free assay)	5-HT7 receptor ^[1] (Cell-free assay)	D2 receptor ^[1] (Cell-free assay)	5-HT1A receptor ^[1] (Cell-free assay)
0.5 nM(Ki)	0.5 nM(Ki)	1 nM(Ki)	6.4 nM(Ki)

In Vitro
In vitro	Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D2 and serotonin 5-HT2A receptors, and is a partial agonist at 5-HT1A receptors. It has much greater affinity for 5-HT7 subtype receptors than other atypical antipsychotics. Lurasidone also has high affinity for the 5-HT1A subtype, α2c-adrenergic receptors and low affinity for α1-adrenergic receptors. It has minimal affinity for 5-HT2C receptors and negligible affinity for histamine H1 and muscarinic receptors^[2].

In Vivo
In Vivo	Lurasidone is rapidly absorbed, reaching peak concentrations within 1.5–3 hours (tmax) after single and multiple oral doses. Once absorbed, it extensively distributes in tissues and rapidly enters the CNS. Lurasidone has high binding to human plasma albumin and alpha-1-glycoprotein (≥99%)^[2]. Long-term treatment of schizophrenia with lurasidone has been shown to reduce the risk of relapse. The elimination half-life of lurasidone is about 20-40 h. Mean Cmax and area under the curve (AUC) for lurasidone were approximately threefold and twofold greater, respectively, in a comparison of administration with food v. fasting. Lurasidone absorption is independent of food fat content. Lurasidone is metabolised primarily via CYP3A4^[1]. In animal studies, lurasidone penetrated the placental barrier and distributed into the fetus, and was excreted in milk during lactation^[2].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT03627195	Completed	Schizophrenia	Sumitomo Pharma America Inc.	June 7 2018	Phase 1
NCT02731612	Recruiting	Bipolar Disorder	Nazlin Walji\|University of British Columbia	May 8 2017	Phase 3
NCT02147379	Completed	Bipolar I Disorder	University of British Columbia	May 2014	Phase 3
NCT02174523	Completed	Schizophrenia	Sumitomo Pharma (Suzhou) Co. Ltd.\|Xuhui Central Hospital Shanghai	April 2014	Phase 1

参考
[1] Antony Loebel, et al. BJPsych Bull. 2015, 39(5): 237–241. [2] Caccia S, et al. Neuropsychiatr Dis Treat. 2012, 8:155-68.

参考

化学情報

分子量	492.68	化学式	C₂₈H₃₆N₄O₂S
CAS No.	367514-87-2	SDF	--
Smiles	C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 7 mg/mL ( (14.2 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):