hydron;(1S,2S)-2-(methylamino)-1-phenylpropan-1-ol

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: hydron;(1S,2S)-2-(methylamino)-1-phenylpropan-1-ol
• 化学式: C10H16NO+
• 分子量: 166.24
• InChiKey: KWGRBVOPPLSCSI-WCBMZHEXSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  36.8
• 氢给体数：
  2
• 氢受体数：
  1

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：尽管母乳中的伪麻黄碱含量很少，对哺乳婴儿造成伤害的可能性不大，但偶尔可能会引起婴儿易怒。单剂量的伪麻黄碱会急性减少乳汁产生，并且反复使用似乎会干扰哺乳。对于哺乳尚未完全建立的新生儿母亲，或者正在努力产生足够乳汁的母亲，不应接受伪麻黄碱。有报道称，对于乳汁过多的母亲，可以使用伪麻黄碱来减少乳汁供应的治疗方案。 ◉ 对哺乳婴儿的影响：在一项针对哺乳母亲的研究中，有20%的婴儿在接触伪麻黄碱后报告出现易怒。 法国药物警戒中心整理了1985年1月至2011年6月间报告的所有哺乳婴儿的不良反应。在174份报告中，伪麻黄碱被报告为4名婴儿引起不良反应的原因，主要是激动不安。 ◉ 对哺乳和母乳的影响：在8位哺乳母亲单次口服伪麻黄碱60毫克后，接下来的24小时内乳汁产生平均减少了24%。没有检测到乳腺血流量发生变化可以解释乳汁减少；服用伪麻黄碱后，血清催乳素下降了13.5%，但这一变化无统计学意义。未测量催产素水平。

◉ Summary of Use during Lactation:Although the small amounts of pseudoephedrine in breastmilk are unlikely to harm the nursing infant, it may cause irritability occasionally. A single dose of pseudoephedrine decreases milk production acutely and repeated use seems to interfere with lactation. Mothers with newborns whose lactation is not yet well established or in mothers who are having difficulties producing sufficient milk should not receive pseudoephedrine. A treatment scheme has been reported for mothers with hypergalactia that uses pseudoephedrine to decrease milk supply. ◉ Effects in Breastfed Infants:Mothers reported irritability was reported in 20% of infants exposed to pseudoephedrine in one study of breastfeeding mothers. All adverse reactions in breastfed infants reported in France between January 1985 and June 2011 were compiled by a French pharmacovigilance center. Of 174 reports, pseudoephedrine was reported to cause adverse reactions in 4 infants, primarily agitation. ◉ Effects on Lactation and Breastmilk:After a single dose of pseudoephedrine 60 mg orally in 8 nursing mothers, there was a mean 24% decrease in milk production over the following 24 hours. No change in blood flow to the breast was detected that could explain the decreased milk production; there was a 13.5% decrease in serum prolactin after pseudoephedrine, but this change did not achieve statistical significance. Oxytocin levels were not measured.

来源:Drugs and Lactation Database (LactMed)

反应信息

• 作为反应物：
  描述：

  hydron;(1S,2S)-2-(methylamino)-1-phenylpropan-1-ol 、 nicotinamide adenine dinucleotide 生成 (S)-N-methylcathinone 、 氢(+1)阳离子 、 NADH
  参考文献：
  名称：

  摘要：

  DOI：
• 作为产物：
  描述：

  左旋伪麻黄碱 、 在 乙酸乙酯 、 异丙醇 、 (1S,2S)-2-甲氨基-1-苯基丙-1-醇 、 氮 、 1-(5-bromo-1,3-thiazol-2-yl)-1-hydroxyethyl 作用下， 反应 32.33h， 以to afford (1S,2S)-1-hydroxy-N-methyl-1-phenylpropan-2-aminium trans-4-[(1R or 1S)-1-(5-bromo-1,3-thiazol-2-yl)-1-hydroxyethyl]cyclohexanecarboxylate as a white solid的产率得到hydron;(1S,2S)-2-(methylamino)-1-phenylpropan-1-ol
  参考文献：
  名称：

  Aminopyrimidines as Syk inhibitors

  摘要：

  本发明提供了一种新型的嘧啶胺式化合物I，它是脾酪氨酸激酶的有效抑制剂，可用于治疗和预防由该酶介导的疾病，如哮喘、慢性阻塞性肺疾病、类风湿性关节炎和癌症。

  公开号：

  US09290490B2

文献信息

• AMINOPYRIMIDINES AS SYK INHIBITORS
  申请人：Altman Michael D.

  公开号：US20140148474A1

  公开（公告）日：2014-05-29

  The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.

  本发明提供了一种新型的嘧啶胺化合物I，它们是脾脏酪氨酸激酶的有效抑制剂，并可用于治疗和预防由该酶介导的疾病，如哮喘、慢性阻塞性肺病、类风湿性关节炎和癌症。
• Combination dosage form comprising cetirizine and pseudoephedrine
  申请人：PFIZER INC.

  公开号：EP0811374A1

  公开（公告）日：1997-12-10

  A dosage form containing cetirizine as an immediate release component and pseudoephedrine or a pharmaceutically acceptable salt thereof as a controlled release component. A portion of the pseudoephedrine can also be incorporated as an immediate release component. The dosage form is free of alcohols having a molecular weight lower than 100 and reactive derivatives thereof.

  一种含有西替利嗪作为速释成分和伪麻黄碱或其药学上可接受的盐作为控释成分的剂型。部分伪麻黄碱也可作为速释成分加入。该剂型不含分子量小于 100 的醇类及其活性衍生物。
• US6171618B1
  申请人：——

  公开号：US6171618B1

  公开（公告）日：2001-01-09
• US6537573B2
  申请人：——

  公开号：US6537573B2

  公开（公告）日：2003-03-25
• [EN] PHARMACEUTICAL FORMULATIONS CONTAINING SOLUBLE DRUGS<br/>[FR] FORMULATIONS PHARMACEUTIQUES CONTENANT DES MÉDICAMENTS SOLUBLES
  申请人：REDDYS LAB LTD DR

  公开号：WO2012068076A2

  公开（公告）日：2012-05-24

  Pharmaceutical compositions providing modified release of water-soluble drugs. In embodiments, a drug, a hydrophilic release rate controlling substance, and a disintegrant are granulated together and granules are used to prepare tablet or capsule dosage forms.