serotonin | 2493-48-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: serotonin
• 英文别名: 2,3-Dihydro-5-hydroxytryptamine；3-(2-aminoethyl)-2,3-dihydro-1H-indol-5-ol
• CAS: 2493-48-3
• 化学式: C₁₀H₁₄N₂O
• 分子量: 178.234
• InChiKey: FIADRAIKXUISOM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  58.3
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Convalent conjugates of biologically-active compounds with amino acids and amino acid derivatives for targeting to physiologically-protected sites
  申请人：Yatvin B. Milton

  公开号：US20070129312A1

  公开（公告）日：2007-06-07

  This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmacokinetically useful levels and also a method of targeting drugs to physiologically protected sites in vivo. Also provided are drug conjugates with an amino acid or derivative thereof for facilitating such targeted drug delivery. The conjugates and methods of this invention provide an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic, neurological, antibiotic, antibacterial, antimycotic, antiviral, antiproliferative or antineoplastic drugs, agents and conjugates, for rapid and efficient introduction of such agents across, e.g., the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of such drugs, agents and conjugates comprising the conjugates of the invention, in the brain and central nervous system and other physiologically-protected sites.

  本发明描述了一种促进药物进入细胞和组织的方法，使其达到在生理保护位点的药代动力学有效水平，并提供了一种在体内将药物定位到生理保护位点的方法。还提供了含有氨基酸或其衍生物的药物共轭物，以促进这种靶向药物传递。与先前已知的其他药物靶向方法相比，本发明的共轭物和方法提供了药物在这些生理保护位点的浓度，可以在系统水平的给药后达到治疗有效水平，这些水平比目前用于达到治疗剂量的水平低得多。该技术适用于精神药物、神经营养药物、神经药物、抗生素、抗菌药物、抗真菌药物、抗病毒药物、抗增殖或抗肿瘤药物、药剂和共轭物，以快速有效地引入这些药剂通过血脑屏障等。此外，本发明提供了一种保留和延长这些药物、药剂和共轭物在大脑和中枢神经系统以及其他生理保护位点中的酶释放的手段，包括本发明的共轭物。
• 2-ALKYL-INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS
  申请人：Alisi Maria Alessandra

  公开号：US20100056573A1

  公开（公告）日：2010-03-04

  2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.

  2-烷基吲唑化合物及其药学上可接受的酸盐，其制备方法和中间体，包含它们的制药组合物以及其用途。2-烷基吲唑化合物具有以下一般式（I），其中R1、R2、R3、R4、R6、R7、X、Y、W、n、p和m的含义如说明中所述。
• 2 -ALKYL- INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS
  申请人：Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.

  公开号：EP2099780A1

  公开（公告）日：2009-09-16
• US8507528B2
  申请人：——

  公开号：US8507528B2

  公开（公告）日：2013-08-13
• [EN] 2 -ALKYL- INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS<br/>[FR] COMPOSÉS DE 2-ALKYL-INDAZOLE POUR LE TRAITEMENT DE CERTAINES AFFECTIONS LIÉES AU SNC
  申请人：ACRAF

  公开号：WO2008061688A1

  公开（公告）日：2008-05-29

  [EN] 2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.
  [FR] La présente invention concerne un composé de 2-alkyl-indazole et ses sels d'addition d'acide pharmaceutiquement acceptables, un procédé et des intermédiaires pour leur préparation, une composition pharmaceutique qui les contient et l'utilisation de cette dernière. Le composé de 2-alkyl-indazole possède la formule générale suivante (I) dans laquelle R¹, R², R³, R⁴, R⁶, R⁷, X, Y, W, n, p et m ont les sens donnés dans la description.