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舒托必利 | 53583-79-2

中文名称
舒托必利
中文别名
舒多必利;吡乙磺苯酰胺;N-[(1-乙基-吡咯烷基)甲基]-5-(乙基磺酰基)-2-甲氧基苯甲酰胺盐酸盐
英文名称
sultopride
英文别名
(+/-)-Sultopride;Barnetil;5-ethanesulfonyl-N-(1-ethyl-pyrrolidin-2-ylmethyl)-2-methoxy-benzamide;N-[(1-ethylpyrrolidin-2-yl)methyl]-5-(ethylsulfonyl)-2-methoxybenzamide;N-(1-Ethyl-2-pyrrolidylmethyl)-2-methoxy-5-ethylsulfonyl-benzamid;N-(1-Ethyl-2-pyrrolidylmethyl)-2-methoxy-5-ethylsulfonylbenzamid;N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide
舒托必利化学式
CAS
53583-79-2
化学式
C17H26N2O4S
mdl
——
分子量
354.47
InChiKey
UNRHXEPDKXPRTM-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

物化性质

  • 熔点:
    181-182 °C
  • 沸点:
    530.0±50.0 °C(Predicted)
  • 密度:
    1.1814 (rough estimate)
  • 溶解度:
    溶于二甲基亚砜
  • 保留指数:
    3065;3036.1

计算性质

  • 辛醇/水分配系数(LogP):
    1.6
  • 重原子数:
    24
  • 可旋转键数:
    7
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    0.59
  • 拓扑面积:
    84.1
  • 氢给体数:
    1
  • 氢受体数:
    5

ADMET

毒理性
  • 在妊娠和哺乳期间的影响
哺乳期使用概要:阿米舒必利进入母乳的量比其他药理上相似的药物要高。关于阿米舒必利的大部分信息是作为精神治疗药物持续口服使用。对于这些用途,可能更倾向于使用替代药物,特别是在哺乳新生儿或早产儿时。对于手术后恶心和呕吐的单次剂量,制造商建议在恢复哺乳前等待48小时;然而,由于半衰期为4到5小时,等待12到24小时应该足够避免大量药物进入母乳。 对哺乳婴儿的影响:一名13个月大的婴儿部分由一名正在服用阿米舒必利400毫克、伏沙明200毫克和硫唑嘌呤150毫克每日的母亲哺乳,并且该母亲正在使用尼古丁口香糖来戒烟。母亲服用阿米舒必利已有9天;其他药物的服用时长未说明。儿科检查发现婴儿发育良好。 一名长期患有精神分裂症的女性在怀孕的大部分期间和哺乳期间(具体程度未说明)接受了阿米舒必利400毫克和氯丙嗪5毫克的治疗。儿科医生对哺乳婴儿进行了13个月的随访,未发现不良反应,婴儿发育正常。 对泌乳和母乳的影响:阿米舒必利会增加血清催乳素平,并可能比其他精神药物更频繁地导致乳汁分泌过多。在已建立泌乳的母亲中,催乳素平可能不会影响她的哺乳能力。
◉ Summary of Use during Lactation:Excretion of amisulpride into breastmilk is higher than with other pharmacologically similar drugs. Most information on amisulpride is with continuous oral use as a psychotherapeutic agent. For these uses, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. After a single dose for post-operative nausea and vomiting, the manufacturer suggests waiting 48 hours before resuming breastfeeding; however, with a half-life of 4 to 5 hours, a waiting period of 12 to 24 hours should be adequate to avoid large amounts being excreted into breastmilk. ◉ Effects in Breastfed Infants:A 13-month-old infant was partially breastfed by a mother who was taking amisulpride 400 mg, fluvoxamine 200 mg, and azathioprine 150 mg daily, and was using nicotine chewing gum for smoking cessation. The mother had been taking amisulpride for 9 days; the duration of the other medications was not stated. A pediatric examination found the infant to be developing well. A woman with long-standing schizophrenia was treated with amisulpride 400 mg and haloperidol 5 mg daily throughout most of her pregnancy and during breastfeeding (extent not stated). Follow-up of the breastfed infant for 13 months by a pediatrician found no adverse effects and normal development of the infant. ◉ Effects on Lactation and Breastmilk:Amisulpride increases serum prolactin and may cause galactorrhea at a higher rate than other psychotropic drugs. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
来源:Drugs and Lactation Database (LactMed)

安全信息

  • 海关编码:
    2933990090
  • 储存条件:
    2-8℃

SDS

SDS:3cd78c5e6839ade0d282f8a1dc86fa9b
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制备方法与用途

Sultopride是一种选择性的多巴胺受体拮抗剂。

文献信息

  • [EN] COMT INHIBITING METHODS AND COMPOSITIONS<br/>[FR] PROCÉDÉS D'INHIBITION DE LA COMT ET COMPOSITIONS ASSOCIÉES
    申请人:LIEBER INST FOR BRAIN DEV
    公开号:WO2016123576A1
    公开(公告)日:2016-08-04
    The present inventions include a method of inhibiting COMT enzyme in a subject as well as compounds of formula I, or a pharmaceutically acceptable salt thereof, that are useful in the treatment of various disorders mediated by COMT, including Parkinson's disease and/or schizophrenia.
    这些发明包括一种抑制受试者中COMT酶的方法,以及式I的化合物或其药用可接受盐,这些化合物在治疗由COMT介导的各种疾病中有用,包括帕森病和/或精神分裂症。
  • METHODS AND SYSTEMS FOR DESIGNING AND/OR CHARACTERIZING SOLUBLE LIPIDATED LIGAND AGENTS
    申请人:TUFTS MEDICAL CENTER
    公开号:US20160052982A1
    公开(公告)日:2016-02-25
    The present application provides methods for preparing soluble lipidated ligand agents comprising a ligand entity and a lipid entity, and in some embodiments, provides relevant parameters of each of these components, thereby enabling appropriate selection of components to assemble active agents for any given target of interest.
    本申请提供了制备可溶性脂质化配体药剂的方法,包括配体实体和脂质实体,并在某些实施例中提供了这些组分的相关参数,从而使得能够适当选择组分来组装出针对任何感兴趣的靶点的活性药剂。
  • [EN] PYRAZOLO [4, 3-D] PYRIMIDINES USEFUL AS KINASE INHIBITORS<br/>[FR] PYRAZOLO[4,3-D]PYRIMIDINES UTILES EN TANT QU'INHIBITEURS DE KINASES
    申请人:ORIGENIS GMBH
    公开号:WO2012143144A1
    公开(公告)日:2012-10-26
    The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    本发明涉及一种能够抑制一个或多个激酶,特别是SYK(脾酪氨酸激酶)、LRRK2(富含亮酸重复的激酶2)和/或MYLK(肌球蛋白轻链激酶)或其突变体的化合物的新颖化合物(I)的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。
  • Hydroxylated nebivolol metabolites
    申请人:O'Donnell P. John
    公开号:US20070014733A1
    公开(公告)日:2007-01-18
    Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.
    羟基化奈必洛尔代谢物在急性给药后以浓度依赖性方式增加人内皮细胞制剂的一氧化氮释放。此外,羟基化奈必洛尔代谢物,包括但不限于4-羟基-6,6'-二代-、4-羟基-5-苯酚-6,6'-二代-和4-羟基-8-苯并-6,6'-二代-,在慢性给药后能够增加人内皮细胞的一氧化氮释放能力。本发明提供了羟基化奈必洛尔代谢物和包含奈必洛尔和/或至少一种羟基化奈必洛尔代谢物和/或至少一种用于治疗心血管疾病的附加化合物的组合物,以及可药用的盐。此外,本发明还提供了通过给药至少一种能够释放治疗有效量的一氧化氮到受血管疾病影响的靶向部位的羟基化奈必洛尔代谢物来治疗和/或预防血管疾病的方法。本发明还涉及通过给药至少一种羟基化奈必洛尔代谢物来治疗和/或预防偏头痛。本发明还可以与治疗代谢综合征障碍的其他治疗联合使用,或作为单一治疗。
  • Nitric Oxide Releasing Prodrugs of Therapeutic Agents
    申请人:SATYAM Apparao
    公开号:US20110263526A1
    公开(公告)日:2011-10-27
    The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.
    本发明涉及已知药物或治疗剂的一氧化氮释放前药,其在此处表示为式(I)的化合物,其中药物或治疗剂包含一个或多个功能基团,独立地选自羧酸基、羟基和巯基。该发明还涉及制备一氧化氮释放前药(式(I)的化合物)的方法,含有它们的药物组合物以及使用这些前药的方法。
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