(1R,2S,6R,14R,15R,19R)-19-[(2S)-2-hydroxypentan-2-yl]-15-methoxy-5-methyl-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11,16-tetraen-11-ol | 14521-96-1

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: (1R,2S,6R,14R,15R,19R)-19-[(2S)-2-hydroxypentan-2-yl]-15-methoxy-5-methyl-13-oxa-5-azahexacyclo[13.2.2.12,8.01,6.02,14.012,20]icosa-8(20),9,11,16-tetraen-11-ol
• CAS: 14521-96-1
• 化学式: C₂₅H₃₃NO₄
• 分子量: 411.5
• InChiKey: CAHCBJPUTCKATP-NNFUYEGGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.68
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  5

ADMET

毒理性

• 解毒与急救

紧急和支持性措施：保持呼吸道通畅，必要时辅助呼吸。给予补充氧气。如果出现昏迷、癫痫、低血压和非心源性肺水肿，则进行治疗。/阿片类药物和阿片样物质/

Emergency and supportive measures: Maintain an open airway and assist ventilation if necessary. Administer supplemental oxygen. Treat coma, seizures, hypotension, and noncardiogenic pulmonary edema if they occur. /Opiates and opioids/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

特定药物和解毒剂：纳洛酮是一种特异性的阿片类药物拮抗剂，本身没有激动剂特性；可以安全地给予大剂量。 ... 注意：纳洛酮的作用持续时间（1-2小时）短于许多阿片类药物。因此，在最后一次给予纳洛酮后至少经过3-4小时之前，不要释放已经苏醒的病人。通常情况下，如果需要纳洛酮来逆转阿片类药物引起的昏迷，将病人留院观察至少6-12小时更为安全。纳美芬是一种作用持续时间更长的阿片类药物拮抗剂（3-5小时）。 ... /阿片类药物和鸦片类物质/

Specific drugs and antidotes: Naloxone is a specific opioid antagonist with no agonist properties of its own; large doses may be given safely. ... Caution: The duration of effect of naloxone (1-2 hours) is shorter than that of many opioids. Therefore, do not release a patient who has awakened after naloxone treatment until at least 3-4 hours has passed since the last dose of naloxone. In general, if naloxone was required to reverse opioid-induced coma, it is safer to admit the patient for at least 6-12 hours of observation. Nalmefene is an opioid antagonist with a longer duration of effect (3-5 hours). ... /Opiates and opioids/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

解毒。如果条件适当，口服活性炭。在小到中等量摄入后，如果能及时给予活性炭，则无需进行洗胃。... /阿片类药物和镇痛剂/

Decontamination. Administer activated charcoal orally if conditions are appropriate. Gastric lavage is not necessary after small to moderate ingestions if activated charcoal can be given promptly. ... /Opiates and opioids/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

增强消除。由于阿片类药物的分布量非常大，且存在有效的解毒治疗方法，因此增强消除程序没有作用。/阿片类药物和鸦片类药物/

Enhanced elimination. Because of the very large volumes of distribution of the opioids and the availability of an effective antidotal treatment, there is no role for enhanced elimination procedures. /Opiates and opioids/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

人体暴露研究/ 酮基芬，一种强效的吗啡样药物，其效果与吗啡进行了定性和定量比较。在非依赖性受试者中，酮基芬的剂量为0.025、0.050和0.100毫克时，能产生瞳孔收缩和类似吗啡的主观效果以及欣快感。酮基芬的效力是吗啡的500倍，具有非常快速的作用发作和短暂的作用持续时间。在吗啡依赖性受试者中，酮基芬抑制了戒断症状，但持续时间比吗啡短。这些研究表明，在人体中，酮基芬是一种具有高滥用潜力的类似吗啡的药物。

/HUMAN EXPOSURE STUDIES/ The effects of etorphine, a potent morphine-like drug, were qualitatively and quantitatively compared to those of morphine. In nondependent subjects, etorphine in doses of 0.025, 0.050, and 0.100 mg produced pupillary constriction and morphine-like subjective effects and euphoria. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. These studies indicate that in man etorphine is a morphine-like drug with a high abuse potential.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

11头幼年非洲象被给予盐酸埃托啡（2.19 ± 0.11微克/千克体重；平均值 ± 标准差）作为单次肌内注射；3头大象额外给予了埃托啡（0.42 ± 0.09微克/千克）静脉注射。在麻醉后，每头大象通过给予0.5%的氟烷/氧气混合物或者多次静脉注射埃托啡来维持侧卧位。在注射后0.25小时和0.5小时以及此后每30分钟，通过耳动脉收集血液样本，并使用放射免疫分析测定埃托啡的血清浓度。在单次肌内注射并随后用氟烷和氧气维持的6头大象中，埃托啡的最高平均血清浓度在注射后0.5小时为1.62 ± 0.97纳克/毫升；此后，平均血清浓度稳步下降。在用多次静脉注射埃托啡维持侧卧位的4头大象中，没有发现觉醒初期征兆出现时间与觉醒前埃托啡血清浓度之间的相关性。在给予初步麻醉剂量的埃托啡后，静脉注射埃托啡的间隔时间缩短。/盐酸埃托啡/

Eleven juvenile African elephants were given etorphine hydrochloride (2.19 +/- 0.11 micrograms/kg of body weight; mean +/- SD) as a single IM injection; 3 elephants were given additional etorphine (0.42 +/- 0.09 micrograms/kg) IV. After immobilization, each elephant was maintained in lateral recumbency by administration of a 0.5% halothane/oxygen mixture or by administration of multiple IV injections of etorphine. At postinjection hours 0.25 and 0.5 and at 30-minute intervals thereafter, blood samples were collected via an auricular artery, and serum concentrations of etorphine were determined by use of radioimmunoassay. The highest mean serum concentration of etorphine in 6 elephants given a single IM injection and subsequently maintained on halothane and oxygen was 1.62 +/- 0.97 ng/mL at postinjection hours 0.5; thereafter, the mean serum concentration decreased steadily. In 4 elephants maintained in lateral recumbency with multiple IV administrations of etorphine, a correlation was not found between the time to develop initial signs of arousal and serum concentrations of etorphine before arousal. After administration of the initial immobilizing dose of etorphine, the interval between successive IV administrations of etorphine decreased. /Etorphine hydrochloride/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在一个涉及Immobilin商业配方的法医案例中，死后采集的股静脉和心脏血液标本中测得的埃托啡浓度分别为14.5和23.5微克/升。尿液中未检测到埃托啡。

In a forensic case involving Immobilon /commerical formulation/, the etorphine concentrations measured in postmortem femoral vein and heart blood specimens were 14.5 and 23.5 ug/L, respectively. No etorphine was detected in the urine.

来源:Hazardous Substances Data Bank (HSDB)