海蒽酮甲磺酸盐 | 23255-93-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 硫色烯
• 中文名称: 海蒽酮甲磺酸盐
• 中文别名: 甲磺酸海蒽酮
• 英文名称: Hycanthone mesylate
• 英文别名: 1-[2-(diethylamino)ethylamino]-4-(hydroxymethyl)thioxanthen-9-one;methanesulfonic acid
• CAS: 23255-93-8
• 化学式: C21H28N2O5S2
• 分子量: 452.6
• InChiKey: LOEQGPPJCCUXEJ-UHFFFAOYSA-N

物化性质

• 物理描述：
  Hycanthone methanesulfonate is an odorless yellow to yellow-orange powder. Bitter taste. (NTP, 1992)
• 颜色/状态：
  Yellow-orange powder
• 熔点：
  approx 143 °C
• 溶解度：
  greater than or equal to 100 mg/mL at 70° F (NTP, 1992)
• 稳定性/保质期：

  This chemical is sensitive to light. A 10% solution in water is stable for at least 24 hours after preparation. It decomposes rapidly in aqueous acid solutions.

• 分解：
  When heated to decomp it emits very toxic fumes of /nitrogen oxides and sulfur oxides/. /Hycanthone/

计算性质

• 辛醇/水分配系数(LogP)：
  1.41
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  145
• 氢给体数：
  3
• 氢受体数：
  7

ADMET

代谢

在雄性Sprague-Dawley大鼠和两种性别恒河猴单次肌肉注射随机三氚标记的硫化羟钴胺酸盐后，血液和组织中达到峰值水平的时间大约在给药后30-60分钟，所用剂量是人类治疗推荐范围（3毫克/千克体重）之内。除了在大鼠肝脏中迅速转化为羟钴胺磺氧化物，在猴子的肝脏中转化为N-脱乙基代谢物之外，血液和组织中发现了未改变的药物。

In male Sprague-Dawley rats and in rhesus monkeys of both sexes receiving single im injections of randomly tritiated hycanthone mesylate at doses in the range of those therapeutically recommended for man (3 mg/kg bw), peak blood and tissue levels were found about 30-60 minutes after administration. ... Unchanged drug was found in blood and tissues, except in the liver where rapid conversion to hycanthone sulphoxide occured in rats and to the N-de-ethylated metabolite in monkeys.

来源:Hazardous Substances Data Bank (HSDB)

代谢

标记的苦艾素排泄速率已在三种大鼠（Sprague-Dawley、带头巾的和Gunn）的胆汁和尿液中以及狗、猫、兔子和猴子的胆汁和尿液中确定。...胆汁和尿液中的大部分放射性物质以结合形式存在，或者是极性代谢物；然而，猫尿液中含有较高百分比的苦艾素和较少的极性代谢物。在胆汁和/或尿液中已观察到大约十五种代谢物，以及通过体外与微粒体制剂孵育产生的九种代谢物。其中五种，包括苦艾素，已经通过化学手段进行了特征描述，另外两种代谢物暂时被识别。

The rate of excretion of labelled hycanthone has been determined in bile and urine from three strains of rats (Sprague-Dawley, hooded and Gunn), and from dogs, cats, rabbits and monkeys. ... Most of the radioactivity in the bile and urine was found in conjugated form, or as polar metabolites; cat urine, however contained a high percentage of hycanthone and less polar metabolites. Some fifteen metabolites have been seen in bile, and/or urine, and nine from in vitro incubations with microsomal preparations. Five of these, including hycanthone, have been chemically characterized, and two others tentatively identified.

来源:Hazardous Substances Data Bank (HSDB)

代谢

在雄性 Sprague-Dawley 大鼠和两种性别的恒河猴单次肌肉注射随机标记的三氢化氢酸甲磺酸盐，剂量范围为人治疗推荐量（3 mg/kg 体重）时，给药后约30-60分钟达到血液和组织中的峰值水平。...除了在大鼠肝脏中迅速转化为氢酸磺氧化物和在猴中转化为N-脱乙基代谢物外，血液和组织中发现了未改变的药物。

In male Sprague-Dawley rats and in rhesus monkeys of both sexes receiving single im injections of randomly tritiated hycanthone mesylate at doses in the range of those therapeutically recommended for man (3 mg/kg bw), peak blood and tissue levels were found about 30-60 minutes after administration. ... Unchanged drug was found in blood and tissues, except in the liver where rapid conversion to hycanthone sulphoxide occured in rats and to the N-de-ethylated metabolite in monkeys.

来源:Hazardous Substances Data Bank (HSDB)

代谢

标记的羟基咔唑的排泄速率已经在三种大鼠（Sprague-Dawley、带头巾的和Gunn）的胆汁和尿液中以及狗、猫、兔子和猴子的胆汁和尿液中确定。...胆汁和尿液中的大部分放射性物质以结合形式存在，或者是极性代谢物；然而，猫尿液中含有较高百分比的羟基咔唑和较少的极性代谢物。在胆汁和/或尿液中已经观察到了大约十五种代谢物，以及通过体外与微粒体制剂孵育得到的九种代谢物。其中五种，包括羟基咔唑，已经通过化学手段进行了表征，另外两种代谢物暂时被识别。

The rate of excretion of labelled hycanthone has been determined in bile and urine from three strains of rats (Sprague-Dawley, hooded and Gunn), and from dogs, cats, rabbits and monkeys. ... Most of the radioactivity in the bile and urine was found in conjugated form, or as polar metabolites; cat urine, however contained a high percentage of hycanthone and less polar metabolites. Some fifteen metabolites have been seen in bile, and/or urine, and nine from in vitro incubations with microsomal preparations. Five of these, including hycanthone, have been chemically characterized, and two others tentatively identified.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌物分类

国际癌症研究机构致癌剂：甲磺酸海葱酮

IARC Carcinogenic Agent:Hycanthone mesylate

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构（IARC）致癌物分类：第3组：无法归类其对人类致癌性

IARC Carcinogenic Classes:Group 3: Not classifiable as to its carcinogenicity to humans

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构专著：第13卷：（1977年）一些杂项药物物质

IARC Monographs:Volume 13: (1977) Some Miscellaneous Pharmaceutical Substances

来源:International Agency for Research on Cancer (IARC)

毒理性

• 相互作用

咖啡因与已知对酿酒酵母（Saccharomyces cerevisiae）减数分裂过程中染色体分离有影响的化学物质的相互作用被研究。看起来咖啡因确实在减数分裂的不同阶段干扰了其他化合物的作用。使用甲基甲磺酸（MMS）和氯化镉（CdCl2）的处理产生了协同效应，包括重组频率的增加。在诱导二倍体孢子方面发现了最大的影响：MMS、海葱酮和地斯塔霉素显示出强烈的协同作用，而苯菌灵的协同作用则较小。关于二体诱导：当使用MMS和海葱酮时，咖啡因减少了（或未改变）非分离的影响。/未指明盐分/

Interactions of caffeine with chemicals known for their effects on chromosomal segregation during meiosis of Saccharomyces cerevisiae were studied. It appears that caffeine does interfere with the action of other compounds during the different phases of meiosis. Treatments with methyl methanesulphonate (MMS) and cadmium chloride (CdCl2) resulted in a synergistic effect consisting of an increase in the frequency of recombination. The greatest effects were found on the induction of diploid spores: MMS, hycanthone, and distamycin demonstrated strong, benlate little synergistic action. ...Concerning disomic induction: caffeine reduced (or left unchanged) the effect on non-disjunction when MMS and hycanthone were used. /Salt not specified/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

皮肤接触：立即用大量清水冲洗受影响的皮肤，同时脱去并隔离所有被污染的衣物。用肥皂和清水彻底清洗所有受影响的皮肤区域。如果出现红斑或刺激等症状，立即呼叫医生，并准备将受害者送往医院接受治疗。

SKIN CONTACT: IMMEDIATELY flood affected skin with water while removing and isolating all contaminated clothing. Gently wash all affected skin areas thoroughly with soap and water. If symptoms such as redness or irritation develop, IMMEDIATELY call a physician and be prepared to transport the victim to a hospital for treatment.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在雄性Sprague-Dawley大鼠和两种性别恒河猴单次肌肉注射随机三标硫化氢酸美司钠，剂量范围为人治疗推荐剂量（3毫克/千克体重）时，给药后约30-60分钟达到血液和组织峰值水平。在肝脏、脾脏、肾脏和肾上腺中观察到最高浓度，但在48-72小时内降至给药剂量的<20%。除了在肝脏中大鼠迅速转化为硫化氢氧化物，在猴子中转化为N-脱乙基代谢物外，血液和组织中发现了未改变的药物。

In male Sprague-Dawley rats and in rhesus monkeys of both sexes receiving single im injections of randomly tritiated hycanthone mesylate at doses in the range of those therapeutically recommended for man (3 mg/kg bw), peak blood and tissue levels were found about 30-60 minutes after administration. Highest concentrations were observed in the liver, spleen, kidneys and adrenals but decreased to <20% of the administered dose in 48-72 hr. Unchanged drug was found in blood and tissues, except in the liver where rapid conversion to hycanthone sulphoxide occured in rats and to the N-de-ethylated metabolite in monkeys.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

标记的苦艾碱的排泄速率已经在三种大鼠（Sprague-Dawley、有帽和Gunn）、狗、猫、兔子和猴子中通过胆汁和尿液确定。在所有物种中，胆汁是主要的排泄途径；总放射性排泄的半衰期范围为1.6到3.0小时。除了在猴子和特别是在猫中，相对较少的放射性物质在尿液中找到。胆汁和尿液中大部分的放射性物质以结合形式或极性代谢物存在；然而，猫尿液中含有高百分比的苦艾碱和较少的极性代谢物。在胆汁和/或尿液中已经看到了大约十五种代谢物，以及通过体外与微粒体制剂培养得到的九种代谢物。其中五种，包括苦艾碱，已经被化学特征化，另外两种代谢物被暂时识别。

The rate of excretion of labelled hycanthone has been determined in bile and urine from three strains of rats (Sprague-Dawley, hooded and Gunn), and from dogs, cats, rabbits and monkeys. Bile was the major route of excretion in all species; the half-life for excretion of total radioactivity ranged from 1.6 to 3.0 hours. Relatively little of the radioactivity was found in the urine, except in the monkey and notably in the cat. Most of the radioactivity in the bile and urine was found in conjugated form, or as polar metabolites; cat urine, however contained a high percentage of hycanthone and less polar metabolites. Some fifteen metabolites have been seen in bile, and/or urine, and nine from in vitro incubations with microsomal preparations. Five of these, including hycanthone, have been chemically characterized, and two others tentatively identified.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在雄性Sprague-Dawley大鼠和两种性别恒河猴单次肌肉注射随机三标硫化氢酸美司钠，剂量范围为人治疗推荐剂量（3毫克/千克体重）时，给药后约30-60分钟达到血液和组织峰值水平。在肝脏、脾脏、肾脏和肾上腺中观察到最高浓度，但在48-72小时内降至给药剂量的<20%。除了在肝脏中大鼠迅速转化为硫化氢氧化物，在猴子中转化为N-脱乙基代谢物外，血液和组织中发现了未改变的药物。

In male Sprague-Dawley rats and in rhesus monkeys of both sexes receiving single im injections of randomly tritiated hycanthone mesylate at doses in the range of those therapeutically recommended for man (3 mg/kg bw), peak blood and tissue levels were found about 30-60 minutes after administration. Highest concentrations were observed in the liver, spleen, kidneys and adrenals but decreased to <20% of the administered dose in 48-72 hr. Unchanged drug was found in blood and tissues, except in the liver where rapid conversion to hycanthone sulphoxide occured in rats and to the N-de-ethylated metabolite in monkeys.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

标记的羟基咔唑的排泄速率已经在三种大鼠（Sprague-Dawley、有帽和Gunn）、狗、猫、兔子和猴子中通过胆汁和尿液进行了测定。在所有物种中，胆汁是主要的排泄途径；总放射性排泄的半衰期从1.6到3.0小时不等。除了在猴子和特别是在猫中，相对少量的放射性物质在尿液中找到。胆汁和尿液中大部分的放射性物质以结合形式或极性代谢物存在；然而，猫尿液中含有一高比例的羟基咔唑和较少的极性代谢物。在胆汁和/或尿液中已经观察到了大约十五种代谢物，以及通过微体准备物的体外培养得到的九种代谢物。其中五种，包括羟基咔唑，已经通过化学方法进行了表征，另外两种代谢物暂时被识别。

The rate of excretion of labelled hycanthone has been determined in bile and urine from three strains of rats (Sprague-Dawley, hooded and Gunn), and from dogs, cats, rabbits and monkeys. Bile was the major route of excretion in all species; the half-life for excretion of total radioactivity ranged from 1.6 to 3.0 hours. Relatively little of the radioactivity was found in the urine, except in the monkey and notably in the cat. Most of the radioactivity in the bile and urine was found in conjugated form, or as polar metabolites; cat urine, however contained a high percentage of hycanthone and less polar metabolites. Some fifteen metabolites have been seen in bile, and/or urine, and nine from in vitro incubations with microsomal preparations. Five of these, including hycanthone, have been chemically characterized, and two others tentatively identified.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 海关编码：
  2932999099

文献信息

• Formulation for increasing the weight of livestock, comprising an ionophore and selenium
  申请人：ELI LILLY AND COMPANY

  公开号：EP0671174A2

  公开（公告）日：1995-09-13

  This invention relates to a formulation for increasing weight of livestock comprising an ionophore, selenium and a veterinary acceptable carrier, diluent, excipient and/or adjuvant. The invention also relates to a method of increasing liveweight gain in livestock comprising, administering to said livestock an effective amount of a formulation of the invention. The invention further relates to a method of increasing selenium absorption in livestock comprising, administering to said livestock an effective amount of an ionophore.

  本发明涉及一种用于增加家畜体重的制剂，该制剂由离子体、硒和兽医可接受的载体、稀释剂、赋形剂和/或佐剂组成。本发明还涉及一种增加家畜活重的方法，包括向所述家畜施用有效量的本发明制剂。本发明还涉及一种增加家畜硒吸收的方法，包括向所述家畜施用有效量的离子发酵剂。
• Dosage form, device, and methods of treatment
  申请人：Lowe Barry Lionel

  公开号：US20050064032A1

  公开（公告）日：2005-03-24

  The present invention relates to a controlled dosage release element adapted to be inserted into and retained in the rumen of a ruminant animal. The element comprises: a) one or more discrete and predetermined amounts of at least a first formulation comprising at least a first active agent, the formulation being adapted to dissolve in rumen fluids at a rate such that dissolution of each of the one or more amounts of first formulation provides a short or pulsed episode of release of the first active agent into the rumen; and b) one or more predetermined amounts of at least a second formulation adapted to dissolve at a controlled rate in rumen fluids; wherein the one or more amounts of first formulation are provided at one or more predetermined locations within the element relative to said one or more amounts of second formulation for one or more delayed releases of at least the first active agent into the rumen at predetermined times before, during, after, or any combination thereof, of a predetermined extended time period defined by said second formulation. The invention also relates to a method for delivering at least a first active agent to the rumen of a ruminant animal in a delayed manner at one or more predetermined times after administration to the animal of a composition containing the active agent, the method comprising administering to the animal a controlled dosage release element according to the invention. The first active agent will typically be for the treatment, prophylaxis or both of a diseased or infested state in a ruminant animal, or for altering the physiological status of a ruminant animal.

  本发明涉及一种可插入反刍动物瘤胃并保留在其中的控释元件。该元件包括a) 一种或多种离散和预定量的至少包含第一种活性剂的第一制剂，该制剂在瘤胃液中的溶解速率使第一制剂的每一种或多种量的溶解都能将第一种活性剂短时间或脉冲式地释放到瘤胃中；以及 b) 一种或多种预定量的至少包含第二种制剂的制剂，该制剂在瘤胃液中的溶解速率受控；其中，相对于所述一个或多个量的第二制剂，在元件内的一个或多个预定位置提供一个或多个量的第一制剂，以便在所述第二制剂确定的预定延长时间段之前、期间、之后或其任意组合的预定时间段内，将至少第一活性剂延迟释放到瘤胃中。本发明还涉及一种方法，用于在向反刍动物施用含有活性剂的组合物后，在一个或多个预定时间内，以延迟的方式将至少第一种活性剂输送到反刍动物的瘤胃中，该方法包括向动物施用根据本发明的控释剂。第一种活性剂通常用于治疗、预防或治疗反刍动物的疾病或感染状态，或用于改变反刍动物的生理状态。
• Sustained release capsule and formulations for insertion into rumen
  申请人：ELI LILLY AND COMPANY

  公开号：EP0507629B1

  公开（公告）日：1997-01-22
• DOSAGE FORM, DEVICE AND METHODS OF TREATMENT
  申请人：ELI LILLY AND COMPANY

  公开号：EP1448151A1

  公开（公告）日：2004-08-25
• HERPES VIRUS-BASED COMPOSITIONS AND METHODS OF USE IN THE PRENATAL AND PERINATAL PERIODS
  申请人：THE UNIVERSITY OF ROCHESTER

  公开号：EP1903873A2

  公开（公告）日：2008-04-02