1-(1-苯基环己基)吡咯烷 | 2201-39-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 1-(1-苯基环己基)吡咯烷
• 中文别名: 咯环利定；罗尼环定
• 英文名称: 1-Pyrrolidino-1-phenyl-cyclohexan
• 英文别名: 1-<1-Phenyl-cyclohexyl>-pyrrolidin；Rolicyclidine；1-(1-phenyl-cyclohexyl)-pyrrolidine；PhP；1-(1-phenylcyclohexyl)pyrrolidine
• CAS: 2201-39-0
• 化学式: C₁₆H₂₃N
• 分子量: 229.365
• InChiKey: FYOWWXMGDATDQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

ADMET

毒理性

• 解毒与急救

立即急救：确保已经进行了充分去污。如果患者停止呼吸，开始人工呼吸，最好使用需求阀复苏器、气囊面罩装置或口袋面罩，按训练进行操作。根据需要执行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果发生呕吐，让患者前倾或置于左侧（如果可能的话，头部向下）以保持呼吸道畅通，防止吸入。保持患者安静，维持正常体温。寻求医疗帮助。/失能剂/

Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Incapacitating Agents/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

基本治疗：建立专利气道（如需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。密切观察呼吸不足的迹象，并在必要时辅助通气。通过非重复呼吸面罩以10至15升/分钟的速度给予氧气。监测休克征象，并在必要时进行治疗……预计可能出现癫痫，并在必要时进行治疗……展示友好的态度，并在必要时使用坚定的约束。必须移除区域内的所有危险物品，并将任何可能被吞咽的物品远离患者，因为可能出现奇异的幻觉。对于眼睛污染，立即用水冲洗眼睛。在转运过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……使用快速降温技术来管理高热……不要使用催吐剂。对于摄入，如果患者能够吞咽、有强烈的呕吐反射并不流口水，则用水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释。给予活性炭……/失能剂/

Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations it necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . Demonstrate a friendly attitude and use firm restraint when necessary. All dangerous objects must be removed from the area and anything likely to be swallowed should be kept away from patients, because bizarre delusions may occur. For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Use rapid cooling techniques to manage hyperthermia ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Administer activated charcoal ... . /Incapacitating Agents/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

高级治疗：对于失去意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用带有气囊-阀-面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿...。监测心率和必要时治疗心律失常...。开始静脉输注D5W/SRP：“保持开放”，最小流量/。如果出现低血容量的迹象，使用0.9%生理盐水（NS）或乳酸钠林格液（LR）。对于伴有低血容量迹象的低血压，谨慎给予液体。如果病人在正常血容量时出现低血压，考虑使用血管加压药。注意观察液体过载的迹象...。治疗癫痫或使用镇静剂...，使用地西泮（安定）或劳拉西泮（安定）...。使用丙美卡因氢氯化物协助眼部冲洗...。/致残剂/

Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag-valve-mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Consider vasopressors if patient is hypotensive with a normal fluid volume. Watch for signs of fluid overload ... . Treat seizures or sedate ... with diazepam (Valium) or lorazepam (Ativan) ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Incapacitating Agents/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

这里呈现了一名31岁男性在摄入苯环己基吡咯烷（PHP）后出现神经和精神症状的案例，通过尿液中的PHP检测得到了证实。使用毒扁豆碱（IM）治疗后，这些症状迅速并持续地得到了逆转。

A case is presented of a 31-year-old male who showed neurological and psychic symptoms following ingestion of phenylcyclohexylpyrrolidine (PHP), which was verified by identification of PHP in the urine. Treatment with physostigmine (IM) produced a rapid and sustained reversal of these symptoms.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

二十名表现出精神病的白人男性后来被发现摄入了苯环己基吡咯烷（PHP）。使用5毫克肌注氟哌啶醇治疗导致了显著改善，而安慰剂治疗则没有。氟哌啶醇治疗PHP精神病的结果与之前发布的关于苯环己啶（PCP）精神病的报告相似。

Twenty white males who presented with psychosis were later found to have ingested phenylcyclohexylpyrrolidine (PHP). Treatment with haloperidol 5 mg IM caused significant improvement while placebo treatment did not. Results of haloperidol treatment of PHP psychosis were similar to previously published reports with phencyclidine (PCP) psychosis.

来源:Hazardous Substances Data Bank (HSDB)

反应信息

• 作为产物：
  描述：

  phenylmagnesium bromide 、 1-(1-Pyrrolidin-1-ylcyclohexyl)benzotriazole 以 乙醚 、 苯 为溶剂， 以13%的产率得到1-(1-苯基环己基)吡咯烷
  参考文献：
  名称：

  The Chemistry ofN-Substituted Benzotriazoles; Part II.¹The Preparation of Tertiary Amines Containing Tertiary-Alkyl Groups from Ketones, Secondary Amines, and Organometallic Reagents

  摘要：

  通过格氏试剂与环酮、苯并三唑（或吡唑）和仲胺的加合物反应制备具有重要药用活性的高支链叔胺，其效果远远优于以前的方法。

  DOI：

  10.1055/s-1989-27156

文献信息

• [EN] A NEW CLASS OF MU-OPIOID RECEPTOR AGONISTS<br/>[FR] NOUVELLE CLASSE D'AGONISTES DU RÉCEPTEUR MU-OPIOÏDE
  申请人：UNIV COLUMBIA

  公开号：WO2015138791A1

  公开（公告）日：2015-09-17

  The present invention provides a compound having the structure (I) or a pharmaceutically acceptable salt or ester thereof.

  本发明提供了一种具有结构（I）的化合物或其药用可接受的盐或酯。
• ABUSE DETERRENT AND ANTI-DOSE DUMPING PHARMACEUTICAL SALTS USEFUL FOR THE TREATMENT OF ATTENTION DEFICIT/HYPERACTIVITY DISORDER
  申请人：King Clifford Riley

  公开号：US20120028960A1

  公开（公告）日：2012-02-02

  A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

  一种药物组合物，包括基本上由含有药用活性化合物的胺的药用可接受的有机酸加合盐组成的药物物质，其中含有药用活性化合物的胺被选择自光学异构体或单异构体利他林酸或苯乙胺衍生物的群体，并且该药物物质具有从无定形到多型的物理形式。
• [EN] MITRAGYNINE ALKALOIDS AS OPIOID RECEPTOR MODULATORS<br/>[FR] ALCALOÏDES DE TYPE MITRAGYNINE UTILISÉS COMME MODULATEURS DE RÉCEPTEURS OPIOÏDES
  申请人：UNIV COLUMBIA

  公开号：WO2017165738A1

  公开（公告）日：2017-09-28

  The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.

  本发明提供一种具有以下结构的化合物：或其药用可接受的盐或酯，并通过向受痛苦、抑郁症、情绪障碍或焦虑障碍的对象施用该化合物的方法来治疗患者。
• SAFETY OF PSUEDOEPHEDRINE DRUG PRODUCTS
  申请人：King Clifford Riley

  公开号：US20140178480A1

  公开（公告）日：2014-06-26

  Drug substances comprising a amine containing pharmaceutically active compound, and at least one of an alditol acetal and an aromatic organic acid as an addition salt or an additive.

  含有胺基药用活性化合物的药物物质，以及至少一种醛糖醚和芳香有机酸中的一种作为附加盐或添加剂。
• Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
  申请人：Bristol David William

  公开号：US20080293695A1

  公开（公告）日：2008-11-27

  Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

  包含药用可接受的有机酸盐的药物物质，其中含有药用活性化合物，用于治疗治疗性疾病管理，并在非治疗管理中使用时展现预防性特性。