盐酸甲吡吩嗪 | 1229-35-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 盐酸甲吡吩嗪
• 中文别名: 盐酸甲地嗪
• 英文名称: methdilazine hydrochloride
• 英文别名: NSC 169091；10-(1-methyl-pyrrolidin-3-ylmethyl)-10H-phenothiazine; monohydrochloride；Hydron;10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine;chloride
• CAS: 1229-35-2
• 化学式: C₁₈H₂₀N₂S*ClH
• 分子量: 332.897
• InChiKey: IEISBKIVLDXSMZ-UHFFFAOYSA-N

物化性质

• 熔点：
  187.5-189°
• 溶解度：
  DMSO（少许）、甲醇（少许）、水（少许）
• 物理描述：
  Methdilazine hydrochloride is a white microcrystalline powder with a slight odor. pH (1% aqueous solution) 4.8-6. (NTP, 1992)
• 颜色/状态：
  LIGHT-TAN, CRYSTALLINE POWDER
• 气味：
  SLIGHT, CHARACTERISTIC
• 味道：
  BITTER, ANESTHETIC

计算性质

• 辛醇/水分配系数(LogP)：
  4.66
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  31.8
• 氢给体数：
  1
• 氢受体数：
  3

ADMET

代谢

主要代谢转化部位是肝脏。/抗组胺药/

MAIN SITE OF METABOLIC TRANSFORMATION IS LIVER. /ANTIHISTAMINES/

来源:Hazardous Substances Data Bank (HSDB)

代谢

H1受体拮抗剂是诱导肝微粒体酶的许多药物之一，它们可能促进自身的代谢。/组胺拮抗剂：H1拮抗剂/

H1 blockers are among the many drugs that induce hepatic microsomal enzymes, and they may facilitate their own metabolism. /Histamine Antagonists: H1 Antagonists/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

METHDILAZINE HYDROCHLORIDE (3 MG/KG IP) POTENTIATED THE PENTOBARBITONE INDUCED HYPNOSIS IN RATS. 盐酸美替拉嗪（3毫克/千克 IP）增强了戊巴比妥诱导的大鼠催眠作用。

METHDILAZINE HYDROCHLORIDE (3 MG/KG IP) POTENTIATED THE PENTOBARBITONE INDUCED HYPNOSIS IN RATS.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

与酒精或其他产生中枢神经系统抑制的药物同时使用可能会增强这些药物或抗组胺药的中枢神经系统抑制作用；此外，与马普替林或三环类抗抑郁药同时使用可能会增强抗组胺药或这些药物的的抗胆碱能效果。/抗组胺药，吩噻嗪衍生物/

Concurrent use /with alcohol or other CNS depression-producing medications/ may potentiate the CNS depressant effects of either these medications or antihistamines; also, concurrent use of maprotiline or tricyclic antidepressants may potentiate the anticholinergic effects of either antihistamines or these medications. /Antihistamines, phenothiazine-derivative/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

与安非他命同时使用可能会降低安非他命的兴奋作用，因为吩噻嗪衍生物产生α-肾上腺素能阻滞。/抗组胺药，吩噻嗪衍生物/

Concurrent use /with amphetamines/ may decrease stimulant effects of amphetamines since phenothiazine derivatives produce alpha-adrenergic blockage. /Antihistamines, phenothiazine-derivative/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

抗胆碱能作用在使用抗组胺药时可能会增强，特别是当同时使用具有抗胆碱能活性的抗胆碱药或其他药物；患者应被告知及时报告胃肠道问题，因为在使用联合疗法时可能会发生麻痹性肠梗阻。/抗组胺药，吩噻嗪衍生物/

Anticholinergic effects may be potentiated when /anticholinergics or other medications with anticholinergic activity/ are used concurrently with antihistamines; patients should be advised to report occurrence of gastrointestinal problems promptly since paralytic ileus may occur with concurrent therapy. /Antihistamines, phenothiazine-derivative/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

对于抗组胺药中毒没有特定的治疗方法，治疗主要是根据一般的对症和支持性措施。如果呼吸衰竭，机械通气支持是维持呼吸比使用容易引起或加剧惊厥阶段的兴奋剂更安全、更有效的手段。/抗组胺药/

THERE IS NO SPECIFIC THERAPY FOR ANTIHISTAMINE POISONING, AND TREATMENT IS ALONG GENERAL SYMPTOMATIC AND SUPPORTIVE LINES. ... SHOULD BREATHING FAIL, MECH SUPPORT OF VENTILATION OFFER SAFER AND ... EFFECTIVE MEANS OF MAINTAINING RESP THAN USE OF ANALEPTICS WHICH ARE PRONE TO INITIATE OR INTENSIFY CONVULSIVE PHASE. /ANTIHISTAMINES/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

口服吸收良好。/抗组胺药，吩噻嗪衍生物/

Well absorbed after oral administration. /Antihistamines, phenothiazine-derivative/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

H1受体拮抗剂从胃肠道吸收良好。口服给药后，血浆浓度在2到3小时内达到峰值，效果通常持续4到6小时；然而，一些药物的药效持续更长时间...。/组胺拮抗剂：H1受体拮抗剂/

The H1 antagonists are well absorbed from the GI tract. Following oral administration, peak plasma concn are achieved in 2 to 3 hr and effects usually last 4 to 6 hr; however, some of the drugs are much longer acting ... . /Histamine Antagonists: H1 Antagonists/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

H1拮抗剂在儿童体内的消除速度比成人快，而在严重肝病患者体内的消除速度则较慢。/组胺拮抗剂：H1拮抗剂/

... H1 antagonists are eliminated more rapidly by children than by adults and more slowly in those with severe liver disease. /Histamine Antagonists: H1 Antagonists/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 海关编码：
  2934300000

制备方法与用途

盐酸甲地嗪是一种口服活性抗生素（组胺拮抗剂），能在体内外抑制多种分枝杆菌，其最低抑菌浓度(MIC)范围为5-15μg/mL，适用于传染病研究[1][2]。

反应信息

• 作为反应物：
  描述：

  甲吡吩嗪 、 盐酸甲吡吩嗪 、 trimeprazine tartarate 生成 盐酸赛庚啶
  参考文献：
  名称：

  Linkage of agents using microparticles

  摘要：

  提供了一种方法、产品和套件，可通过内源或外源性谷氨酰胺转移酶使用微粒子将药剂附着到皮肤表面。

  公开号：

  US20060110379A1

文献信息

• TERPENE COUPLING CONJUGATE
  申请人：LABORATOIRES ERIGER

  公开号：US20210361771A1

  公开（公告）日：2021-11-25

  The subject matter of the present invention relates to the use of an optionally branched linear terpene having at most one C═C unsaturation for the production of conjugates provided with self-assembly properties, as well as a self-assembly agent of formula (I): X(-Spacer-Y-Terpene) p (I) in which: “Terpene” is linear, optionally branched, having at most one C═C unsaturation; “Y” is a bond or a molecular fragment with a biodegradable bond; “Spacer” is a bond or a fragment comprising at least one carbon atom; “X” is a molecular fragment comprising at least one biodegradable bond; “p” ranges between 0.1 and 4; and the “-Spacer-Y-” group optionally can be a bond, as well as the conjugate resulting from the combination of the self-assembly agent of formula (I) with an active molecule MA.

  本发明的主题涉及使用最多具有一个C═C不饱和度的线性可选择分支的萜烯，用于具有自组装特性的共轭物的生产，以及具有以下式(I)的自组装剂： X(-Spacer-Y-Terpene) p (I) 其中： “萜烯”是线性的，可选择分支的，最多具有一个C═C不饱和度； “Y”是一个具有可生物降解键的键或分子片段； “Spacer”是一个包含至少一个碳原子的键或片段； “X”是一个包含至少一个可生物降解键的分子片段； “p”范围在0.1至4之间；以及 “-Spacer-Y-”基团可以选择是一个键， 以及由式(I)的自组装剂与活性分子MA的组合产生的共轭物。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• Dendrimers as molecular translocators
  申请人：Goodman Murray

  公开号：US20060216265A1

  公开（公告）日：2006-09-28

  Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.

  转运分子包括一种树枝状聚合物和一种生物活性分子。这些转运分子的树枝状聚合物包括至少一个胍基团、至少一个质子化的胍基团、至少一个保护的胍基团、至少一个酰胺基团、至少一个质子化的酰胺基团、至少一个保护的酰胺基团、至少一个脲基团、至少一个质子化的脲基团、至少一个保护的脲基团、至少一个硫脲基团、至少一个质子化的硫脲基团，或至少一个保护的硫脲基团。生物活性分子与树枝状聚合物结合。一种增加药物生物利用度的方法包括将药物与本发明的树枝状聚合物结合。
• [EN] NANOPARTICLE FORMULATIONS AND USES THEROF<br/>[FR] FORMULATIONS DE NANOPARTICULES ET LEURS UTILISATIONS
  申请人：ABRAXIS BIOSCIENCE LLC

  公开号：WO2010118365A1

  公开（公告）日：2010-10-14

  The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages.

  本发明提供了包含纳米粒子的组合物，其中包括：1）药物，如疏水性药物衍生物；和2）载体蛋白。还提供了使用这些组合物治疗疾病（如癌症）的方法，以及套件和单元剂量。
• Oligonucleotide compositions and methods for the modulation of the expression of B7 protein
  申请人：——

  公开号：US20040023917A1

  公开（公告）日：2004-02-05

  Compositions and methods for the treatment of asthma with oligonucleotides which specifically hybridize with nucleic acids encoding B7 proteins.

  用与编码B7蛋白的核酸特异杂交的寡核苷酸治疗哮喘的组合物和方法。