Рисперидон
Рисперидон атрибут
Температура плавления: |
170°C |
Температура кипения: |
572.4±60.0 °C(Predicted) |
плотность: |
1.38±0.1 g/cm3(Predicted) |
Fp: |
9℃ |
температура хранения: |
2-8°C |
растворимость: |
ДМСО: ≥5 мг/мл |
пка: |
pKa 8.3 (Uncertain) |
форма: |
пудра |
цвет: |
От белого до не совсем белого |
Растворимость в воде: |
44,74 мг/л (25°С) |
Мерк: |
14,8233 |
BCS Class: |
2 |
Справочник по базе данных CAS: |
106266-06-2(CAS DataBase Reference) |
Словарь онкологических терминов NCI: |
Risperdal; risperidone |
FDA UNII: |
L6UH7ZF8HC |
Код УВД: |
N05AX08 |
безопасность
- Заявления о рисках и безопасности
- код информации об опасности(GHS)
Коды опасности |
T,F |
Заявления о рисках |
25-39/23/24/25-23/24/25-11 |
Заявления о безопасности |
28-36-45-36/37-16 |
РИДАДР |
3249 |
WGK Германия |
3 |
RTECS |
UV1164800 |
Класс опасности |
6.1(a) |
Группа упаковки |
II |
кода HS |
29333990 |
Банк данных об опасных веществах |
106266-06-2(Hazardous Substances Data) |
Токсичность |
LD50 in male, female mice, rats, dogs (mg/kg): 29.7, 26.9, 34.3, 35.4, 14.1, 18.3 i.v.; 82.1, 63.1, 113, 56.6, 18.3, 18.3 orally (Janssen, 1988) |
символ(GHS) |
|
сигнальное слово |
Danger |
Заявление об опасности |
пароль |
Заявление об опасности |
Класс опасности |
категория |
сигнальное слово |
пиктограмма |
предупреждение |
H301 |
Токсично при проглатывании. |
Острая токсичность, пероральная |
Категория 3 |
Опасность |
![](/GHS06.jpg) |
P264, P270, P301+P310, P321, P330,P405, P501 |
|
Внимание |
P301+P310 |
ПРИ ПРОГЛАТЫВАНИИ: Немедленно обратиться за
медицинской помощью. Прополоскать рот. |
|
Рисперидон химические свойства, назначение, производство
Описание
Risperidone is a novel antipsychotic introduced for the treatment of acute and chronic
schizophrenia. It has a balanced serotonin 5-HT2 and dopamine D2 receptor antagonist
activity. While the anti-D2 activity may relate to the antipsychotic potency of neuroleptic
agents, an antidepressive efficacy of substances with anti-5-HT2 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 D2 antagonist antipsychotics.
It also has potential for management of alcohol withdrawal and cocaine addiction.
Химические свойства
Crystalline Solid
Использование
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
Определение
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.
Общее описание
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-HT2–D2 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.
Биологическая активность
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).
Рисперидон препаратная продукция и сырье
сырьё
Иодид калия
Изоксазол
4-Pyrimidinol
1,3-дифторбензол
885706-66-1
Рисперидал iMpurity B
3-(2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride
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
Рисперидон Э-Оксим
2,4-Difluorophenyl-(4-piperidinyl)methanoneoxime
2,4-дифторфенил- (4-пиперидинил) метанон оксим гидрохлорид
6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole
Тетрацианоэтилен
препарат
Рисперидон поставщик
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