リスペリドン 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
用途
ベンゾイソキサザール誘導体 です。ドパミンD2 受容体拮抗作用、セロト ニン5-HT2 受容体拮抗作用を示します。
用途
リスペリドン(英:Risperidone)は、非定型抗精神病薬のひとつである。主に統合失調症の治療に用いられる。
効能
統合失調症治療薬, 神経遮断薬
商品名
リスパダール (ヤンセンファーマ); リスパダール (ヤンセンファーマ); リスパダール (ヤンセンファーマ); リスパダールコンスタ (ヤンセンファーマ)
説明
Risperidone is a novel antipsychotic introduced for the treatment of acute and chronic
schizophrenia. It has a balanced serotonin 5-HT
2 and dopamine D
2 receptor antagonist
activity. While the anti-D
2 activity may relate to the antipsychotic potency of neuroleptic
agents, an antidepressive efficacy of substances with anti-5-HT
2 activity has been
suggested. Risperidone, therefore, has therapeutic action on both positive and negative
symptoms of schizophrenia and produces significantly fewer side effects especially
extrapyramidal symptoms compared with commonly used pure D
2 antagonist antipsychotics.
It also has potential for management of alcohol withdrawal and cocaine addiction.
化学的特性
Crystalline Solid
使用
Risperidone has been used:
- to study its effects on bone formation and differentiation
- to investigate the relationship between risperidone (RIS) dosages and RIS plasma levels in autism spectrum disorder (ASD) pediatric patients
- to reverse induced schizophrenia-like behavior in mice
定義
ChEBI: A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.
一般的な説明
Risperidone (Risperdal, a benzisoxazole)has the structural features of a hybrid molecule between abutyrophenone antipsychotic and a trazodone-like antidepressant.Its superior side effects profile (compared withhaloperidol) at dosage of 6 mg/d or less and the lower riskof tardive dyskinesia have contributed to its very widespreaduse. It benefited refractory psychotic patients, withparkinsonism controlled at one tenth the dose of antiparkinsoniandrugs used with haloperidol.Coexisting anxietyand depressive syndromes were also lessened. It is reportedto decrease the negative (e.g., withdrawal, apathy) as well asthe positive (e.g., delusions, hallucinations) symptoms ofschizophrenia. This is reportedly a consequence of the compound’scombination 5-HT
2–D
2 receptor antagonistic properties.Overall, the reasons for the decreased EPS and effectiveness against negative symptom are still under investigation.It is an important atypical antipsychotic.Risperidone is metabolized in the liver by CYP2D6 to anactive metabolite, 9-hydroxyrisperidone. Because thismetabolite and risperidone are nearly equipotent, the clinicalefficacy of the drug reflects both compounds.
生物活性
Atypical antipsychotic agent that displays 5-HT 2A receptor antagonism. Also displays high affinity at D 2 receptors (K i values are 0.4 and 3.13 nM for 5-HT 2A and D 2 receptors respectively).
リスペリドン 上流と下流の製品情報
原材料
ヨウ化カリウム
イソオキサゾール
ピリミジン-6(1H)-オン
1,3-ジフルオロベンゼン
885706-66-1
Risperidal iMpurity B
3-(2-クロロエチル)-6,7,8,9-テトラヒドロ-2-メチル-4H-ピリド[1,2-a]ピリミジン-4-オン
6-フルオロ-3-(4-ピペリジニル)-1,2-ベンゾイソオキサゾール塩酸塩
3-[2-[4-[(Z)-(2,4-Difluorophenyl)(hydroxyiMino)Methyl]-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2-Methyl-4H-pyrido[1,2-a]pyriMidin-4-one
リスペリドンE-オキシム不純物
2,4-Difluorophenyl-(4-piperidinyl)methanoneoxime
(2,4-ジフルオロフェニル)-4-ピペリジルメタノンオキシム塩酸塩
6-フルオロ-3-(4-ピペリジニル)-1,2-ベンゾイソオキサゾール
テトラシアノエチレン
準備製品