开思酮 | 71031-15-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 开思酮
• 英文名称: cathinone
• 英文别名: (S)-(-)-cathinone；(2S)-2-amino-1-phenylpropan-1-one
• CAS: 71031-15-7
• 化学式: C₉H₁₁NO
• 分子量: 149.192
• InChiKey: PUAQLLVFLMYYJJ-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  43.1
• 氢给体数：
  1
• 氢受体数：
  2

ADMET

代谢

卡西酮通过酮还原代谢成去甲麻黄碱和伪麻黄碱，比例大约为9:1。高达52%的口服剂量的卡西酮异构体在24小时尿液样本中以氨基酸醇代谢物的形式被回收。卡西酮也主要在尿液中排泄：6小时内40%的口服剂量，24小时内84.6%。

Cathinone is metabolized by keto-reduction to norephedrine and norpseudoephedrine at an approximate ratio of 9:1. ... Up to 52% of oral doses of cathinone isomers are recovered in 24 hour urine samples as aminoalcohol metabolites. Cathine is also primarily excreted in the urine: 40% of an oral dose within 6 hours and 84.6% within 24 hours.

来源:Hazardous Substances Data Bank (HSDB)

代谢

口服合成的卡西酮（异构体，外消旋混合物）后，24小时内尿液中回收了22-52%，主要是以氨基酸醇代谢物的形式。通过气相色谱/质谱（GC/MS）、高效液相色谱（HPLC）和圆二色性（CD）分析，S-(-)-卡西酮的主要代谢物被鉴定为R/S-(-)-去甲麻黄碱，而R-(+)-卡西酮的主要代谢物被鉴定为R/R-(-)-去甲伪麻黄碱。这两种氨基酸醇是通过立体特异的酮还原形成的。

... After oral administration of synthesized cathinone (isomers, racemate), 22-52% was recovered in 24 hr urine samples mainly as aminoalcohol metabolites. With GC/MS, HPLC and CD, the main metabolite of S-(-)-cathinone was identified as R/S-(-)-norephedrine and the main metabolite of R-(+)-cathinone as R/R-(-)-norpseudoephedrine. Both aminoalcohols are formed by a stereospecific keto reduction.

来源:Hazardous Substances Data Bank (HSDB)

代谢

Cathinone在肝脏的一级代谢会导致去甲麻黄碱的形成。

First-pass metabolism of cathinone in the liver leads to the formation of norephedrine.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

药物辨别范式被用来评估同时给予咖啡因和尼可刹米对低剂量卡西酮辨别的影响。在训练大鼠在双杠杆食物动机操作任务中辨别0.8 mg/kg l-卡西酮和其载体的实验中，0.2 mg/kg卡西酮产生了29.2%的动物选择卡西酮相应杠杆的反应。在分别给予25 mg/kg尼可刹米和20 mg/kg咖啡因的情况下，选择该杠杆的试验比例分别为0%和50%。同时给予咖啡因、尼可刹米或咖啡因加尼可刹米与低剂量卡西酮，产生了强烈的类似卡西酮的辨别表现。这种咖啡因和尼可刹米增强卡西酮的效果反映了含有类似组合的非受控滥用药物，特别是含有这三种成分的减肥药X-112，这种药物在欧洲被广泛滥用。

The drug discrimination paradigm was employed to evaluate the effect of coadministration of both caffeine and nikethamide upon the discrimination of a low dose of cathinone. In rats trained to discriminate between 0.8 mg/kg l-cathinone and its vehicle in a two-lever food-motivated operant task, 0.2 mg/kg cathinone produced 29.2% of responses on the cathinone-appropriate lever. This lever was chosen in 0 and 50% of trials with 25 mg/kg nikethamide and 20 mg/kg caffeine, respectively. Coadministration of caffeine, nikethamide, or caffeine plus nikethamide with low-dose cathinone produced strong cathinone-like discriminative performance. This potentiattion of cathinone by caffeine and nikethamide is reflective of noncontrolled drugs of abuse containing similar combinations especially for that of antiadipositum X-112, a drug containing all three agents and widely abused in Europe.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

研究了(-)-卡西酮、咖啡因及其组合对雄性大鼠性行为的影响。在没有雌性大鼠的情况下，通过记录勃起反应（生殖器清洁、打哈欠/伸展和同性攀爬）来评估雄性大鼠的性行为。通过将雄性与注射了苯甲酸雌二醇和黄体酮的接受性雌性大鼠放在一起来观察交配行为。记录了雄性大鼠的交配模式（攀爬、插入、射精和不应期）。口服卡西酮（5 mg/kg/天）、咖啡因（50 mg/kg/天）及其组合15天的治疗增加了雄性大鼠的性唤起（动机），表现为攀爬表现和会阴探究行为的增加。然而，本研究中测量的勃起和射精反应没有显示出刺激作用。从目前的结果可以推测，卡西酮（阿拉伯茶中的精神刺激成分）改变了雄性模式行为，而咖啡因在同时给药时也改变了卡西酮的效果。然而，我们的数据没有证据表明卡西酮可以被认为是春药。

The effect of (-)-cathinone, caffeine and their combinations was studied on the sexual behavior of male rats. Male sexual activities were assessed by recording the erectile responses (grooming of genitalis, yawning/stretching and homosexual mounting), in the absence of females. The copulatory behavior was observed by caging males with receptive females brought into oestrus with s.c. injection of estradiol benzoate and progesterone. The copulatory pattern of male rats (mounting, intromissions, ejaculations and refractory period) was recorded. The oral treatment of cathinone (5 mg/kg day), caffeine (50 mg/kg day) and their combinations for 15 days increased arousal (motivation) in male rats as evidenced by increased mounting performance and anogenital investigatory behavior. However, erectile and ejaculatory responses, measured in the present study, showed no stimulant effect. It is conceivable from the present results that cathinone, the psychostimulant constituent of khat modified masculine pattern behavior and caffeine also changed the effect of cathinone when administered concomitantly. However, our data provide no evidence that cathinone could be considered as an aphrodisiac.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

治疗恰特草摄入主要是对症治疗。有症状的患者应置于监测之下，进行心电图检查，并频繁监测生命体征。大多数症状在4到6小时内解决。对于持续生命体征异常、有终末器官缺血证据或精神症状的患者，应入院观察。/恰特草/

Treatment of khat ingestion is largely symptomatic. Symptomatic patients should be placed on a monitor, have an ECG obtained, and have vital signs monitored frequently. Most symptoms resolve in 4 to 6 hours. Patients with persistent vital sign abnormalities, evidence of end-organ ischemia, or psychiatric symptoms should be admitted for observations. /Khat/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 立即急救：确保已经进行了充分的中和。如果患者停止呼吸，请开始人工呼吸，最好使用需求阀复苏器、球囊阀面罩设备或口袋面罩，按训练操作。如有必要，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。如果患者呕吐，让患者向前倾或将其置于左侧（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。寻求医疗救助。 /毒物A和B/

/SRP:/ 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 if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the 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. /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。观察呼吸不足的迹象，如有需要，辅助通气。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，如有必要，进行治疗……。监测休克，如有必要，进行治疗……。预防癫痫发作，如有必要，进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能吞咽、有强烈的干呕反射且不流口水，则用温水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释……。在去污后，用干燥的无菌敷料覆盖皮肤烧伤……。/毒药A和B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . 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 ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

咀嚼卡特叶时，卡特的活性成分通过口腔吸收。卡西酮、卡因和norephedrine的血浆浓度峰值分别在127分钟、183分钟和200分钟达到。

The active components of khat are absorbed orally by chewing the leaves. The peak plasma concentration of cathinone, cathine, and norephedrine are reached in 127 minutes, 183 minutes, and 200 minutes, respectively.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

四名志愿者咀嚼相当于一次典型咀嚼可乐叶活动四分之一的可乐叶。收集了长达80小时的血液样本，并使用气相色谱-质谱法测定了生物碱。数据通过计算机化的药物动力学房室分析进行评估。生物碱的血浆浓度-时间数据可以用具有两段吸收的两个房室模型来描述。口腔粘膜被认为是第一个吸收段，其中大部分生物碱被吸收（对于卡西酮和卡西因，平均±标准差分别为59±21%和84±6%）。通过咀嚼从叶子中提取生物碱的效率非常高，只有9.1±4.2%作为残留物。卡西酮从中央房室中以平均半衰期为1.5±0.8小时被消除。卡西因的半衰期为5.2±3.4小时。卡西酮转化为去甲麻黄碱对其血浆浓度曲线有重大影响。咀嚼可乐叶基本上不影响精神物理功能。

Four volunteers chewed khat leaves in an amount equivalent to one-quarter of that used in a typical khat session. Blood samples were collected up to 80 hr and the alkaloids were assayed using gas chromatography-mass spectrometry. The data were evaluated using computerized pharmacokinetic compartmental analysis. The plasma concentration-time data for the alkaloids could be described using a two-compartment model with two-segment absorption. The mucosa of the oral cavity is considered to be the first absorption segment, where the major proportion of the alkaloids is absorbed (mean +/- SD 59 +/- 21% for cathinone and 84 +/- 6% for cathine). The extraction of the alkaloids from the leaves by chewing was very effective with only 9.1 +/- 4.2% remaining as a residue. Cathinone was eliminated from the central compartment with a mean half-life of 1.5 +/- 0.8 hr. The half-life of cathine was 5.2 +/- 3.4 hr. The metabolism of cathinone to norephedrine had a substantial influence on its plasma concentration profile. Psychophysical functions were essentially unaffected by the chewing of khat.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

卡西酮在血浆中的峰值浓度在开始咀嚼后1.5到3.5小时获得。咀嚼60克新鲜阿拉伯茶一小时后，平均血浆浓度可能达到100纳克/毫升。八小时后，血液中几乎检测不到卡西酮。... 只有2%的卡西酮以原形从尿液中排出。

Peak plasma levels of cathinone are obtained 1.5 to 3.5 hours after the onset of chewing. The mean plasma level may reach 100 ng/mL after chewing 60 g fresh khat for one hour. Cathinone is barely detectable in blood after eight hours. ... Only 2 % of cathinone is excreted unchanged in the urine.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

一小部分卡西酮由肾脏原样排泄（0.6%到3.3%）。

A small amount of cathinone is excreted by thekidney unchanged (0.6% to 3.3%).

来源:Hazardous Substances Data Bank (HSDB)

反应信息

• 作为反应物：
  描述：

  开思酮 在 alcohol dehydrogenase from Ralstonia sp. 作用下， 以 aq. buffer 为溶剂， 以99%的产率得到
  参考文献：
  名称：

  高效的两步生物催化策略，用于合成所有正（伪）麻黄碱异构体

  摘要：

  手性1,2-氨基醇是化学和药学的重要组成部分。在这里，我们开发了两种不同的生物催化两步级联反应，用于合成所有四种正（伪）麻黄碱（N（P）E）立体异构体。在第一个中，（R）选择性硫胺素二磷酸（ThDP）依赖的碳连接酶与（S）或（R）选择性ω-转氨酶的结合导致形成（1 R，2 S）- NE或（1 R，2 R）-NPE具有优异的光学纯度（ee> 99％，de> 98％）。对于（1 R，2 R）-NPE的合成，时空产率高达〜26 g L -1 d -1已经实现。由于目前尚无高度（S）选择性的羰基化酶可用于该反应，因此采用了另一种策略来补充去甲伪麻黄碱平台。在此，（S）-选择性转氨酶与（S）-选择性醇脱氢酶的组合产生（1S，2S）-NPE，其ee＞ 98％且de＞ 99％。尽管冻干的全细胞制备便宜并且显示出适合用作生物催化剂，但是用纯化的酶观察到更高的光学纯度。这些合成酶级联反应使N（P）E产物仅需

  DOI：

  10.1039/c4gc00100a
• 作为产物：
  描述：

  1-苯基-1,2-丙二酮 在 (S)-(-)-N-甲基-1-苯基乙胺 、 Cv-(S)-ω-transaminase 作用下， 以 aq. buffer 为溶剂， 生成 开思酮
  参考文献：
  名称：

  高效的两步生物催化策略，用于合成所有正（伪）麻黄碱异构体

  摘要：

  手性1,2-氨基醇是化学和药学的重要组成部分。在这里，我们开发了两种不同的生物催化两步级联反应，用于合成所有四种正（伪）麻黄碱（N（P）E）立体异构体。在第一个中，（R）选择性硫胺素二磷酸（ThDP）依赖的碳连接酶与（S）或（R）选择性ω-转氨酶的结合导致形成（1 R，2 S）- NE或（1 R，2 R）-NPE具有优异的光学纯度（ee> 99％，de> 98％）。对于（1 R，2 R）-NPE的合成，时空产率高达〜26 g L -1 d -1已经实现。由于目前尚无高度（S）选择性的羰基化酶可用于该反应，因此采用了另一种策略来补充去甲伪麻黄碱平台。在此，（S）-选择性转氨酶与（S）-选择性醇脱氢酶的组合产生（1S，2S）-NPE，其ee＞ 98％且de＞ 99％。尽管冻干的全细胞制备便宜并且显示出适合用作生物催化剂，但是用纯化的酶观察到更高的光学纯度。这些合成酶级联反应使N（P）E产物仅需

  DOI：

  10.1039/c4gc00100a

文献信息

• [EN] SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1<br/>[FR] AGONISTES À PETITES MOLÉCULES DE RÉCEPTEUR DE NEUROTENSINE 1
  申请人：SANFORD BURNHAM MED RES INST

  公开号：WO2014100501A1

  公开（公告）日：2014-06-26

  Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

  提供的是小分子神经降压素受体激动剂，包含这些化合物的组合物，以及使用这些化合物和包含这些化合物的组合物的方法。
• [EN] 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE<br/>[FR] AGONISTES DE RÉCEPTEUR 5-HT2C ET COMPOSITIONS ET PROCÉDÉS D'UTILISATION
  申请人：ARENA PHARM INC

  公开号：WO2017023679A1

  公开（公告）日：2017-02-09

  Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.

  在某些实施例中提供了一些符合本文所定义的A式化合物，其调节5-HT2C受体的活性。在某些实施例中还提供了一些方法，例如用于体重管理、诱导饱腹感、减少食物摄入，以及预防和治疗肥胖、抗精神病药物引起的体重增加、2型糖尿病、普拉德-威利综合征、烟草/尼古丁依赖、药物成瘾、酒精成瘾、病理性赌博、奖赏缺乏综合征和性成瘾，强迫症谱系障碍和冲动控制障碍（包括咬指甲和咬甲症），睡眠障碍（包括失眠、睡眠结构碎裂和慢波睡眠紊乱），尿失禁，精神障碍（包括精神分裂症、厌食症和暴食症），阿尔茨海默病，性功能障碍，勃起功能障碍，癫痫，运动障碍（包括帕金森病和抗精神病药物引起的运动障碍），高血压，血脂异常，非酒精性脂肪肝病，肥胖相关肾脏疾病和睡眠呼吸暂停症。
• SUGAR CHAIN-ATTACHED LINKER, COMPOUND CONTAINING SUGAR CHAIN-ATTACHED LINKER AND PHYSIOLOGICALLY ACTIVE SUBSTANCE OR SALT THEREOF, AND METHOD FOR PRODUCING SAME
  申请人：GLYTECH INC.

  公开号：US20150306235A1

  公开（公告）日：2015-10-29

  To provide a carrier linker that is capable of improving the water solubility of a physiologically active substance and more quickly releasing the physiologically active substance under specific conditions without utilizing light or enzymatic cleavage. [Solution]A novel sugar chain-attached linker comprising a sugar chain that is attached as a carrier.

  提供一种载体连接剂，能够提高生理活性物质的水溶性，并在特定条件下更快地释放生理活性物质，而无需利用光或酶解。【解决方案】一种新型的糖链连接剂，包括作为载体附着的糖链。
• Evaluation of the Edman degradation product of vancomycin bonded to core-shell particles as a new HPLC chiral stationary phase
  作者：Garrett Hellinghausen、Diego A. Lopez、Jauh T. Lee、Yadi Wang、Choyce A. Weatherly、Abiud E. Portillo、Alain Berthod、Daniel W. Armstrong

  DOI：10.1002/chir.22985

  日期：2018.9

  macrocyclic glycopeptide‐based chiral stationary phase (CSP), prepared via Edman degradation of vancomycin, was evaluated as a chiral selector for the first time. Its applicability was compared with other macrocyclic glycopeptide‐based CSPs: TeicoShell and VancoShell. In addition, another modified macrocyclic glycopeptide‐based CSP, NicoShell, was further examined. Initial evaluation was focused on the complementary

  通过对万古霉素的Edman降解制备的修饰的基于大环糖肽的手性固定相（CSP）被首次评估为手性选择剂。将其适用性与其他基于大环糖肽的CSP（TeicoShell和VancoShell）进行了比较。此外，还进一步检查了另一种基于大环糖肽的修饰CSP NicoShell。最初的评估集中在与这些糖肽的互补行为上。根据以前的工作，使用了一种筛选方法，用于对50种手性化合物的对映体分离，其中包括氨基酸，农药，兴奋剂和多种药物。使用表面多孔（核-壳）颗粒载体可实现快速有效的手性分离。总体，万古霉素埃德曼降解产物（EDP）与TeicoShell类似，在极性离子模式下对酸性化合物具有高对映选择性。使用液相色谱-质谱联用EDP同时分离5种外消旋脯氨酸的对映异构体，时间约为3分钟。其他亮点包括同时用VancoShell液相色谱分离rac-amphetamine和rac-methamphetamine，用Nico
• [EN] 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE<br/>[FR] AGONISTES DU RÉCEPTEUR 5-HT2C ET COMPOSITIONS ET PROCÉDÉS D'UTILISATION
  申请人：ARENA PHARM INC

  公开号：WO2015066344A1

  公开（公告）日：2015-05-07

  Provided are 5-HT2C receptor agonists. Also provided are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea. Also provided are compositions comprising a selective 5-HT2C receptor agonist, optionally in combination with a supplemental agent, and methods for reducing the frequency of smoking tobacco in an individual attempting to reduce frequency of smoking tobacco; aiding in the cessation or lessening of use of a tobacco product in an individual attempting to cease or lessen use of a tobacco product; aiding in smoking cessation and preventing associated weight gain; controlling weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; reducing weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; treating nicotine dependency, addiction and/or withdrawal in an individual attempting to treat nicotine dependency, addiction and/or withdrawal; or reducing the likelihood of relapse use of nicotine by an individual attempting to cease nicotine use comprising administering a selective 5-HT2C receptor agonist, optionally in combination with a supplemental agent.

  提供了5-HT2C受体激动剂。还提供了用于体重管理、诱导饱腹感、减少食物摄入量、预防和治疗肥胖、抗精神病药物引起的体重增加、2型糖尿病、普拉德-威利综合征、烟草/尼古丁依赖、药物成瘾、酒精成瘾、病态赌博、奖赏缺乏综合征和性成瘾）、强迫症谱系障碍和冲动控制障碍（包括咬指甲和咬甲）、睡眠障碍（包括失眠、睡眠结构碎裂和慢波睡眠紊乱）、尿失禁、精神障碍（包括精神分裂症、厌食症和暴食症）、阿尔茨海默病、性功能障碍、勃起功能障碍、癫痫、运动障碍（包括帕金森病和抗精神病药物引起的运动障碍）、高血压、血脂异常、非酒精性脂肪肝病、肥胖相关肾脏疾病和睡眠呼吸暂停。还提供了包含选择性5-HT2C受体激动剂的组合物，可选地与辅助剂结合，以及用于减少个体尝试减少吸烟频率的吸烟频率；帮助个体戒除或减少使用烟草制品的个体戒除或减少使用烟草制品；帮助戒烟并预防相关体重增加；通过个体尝试戒烟来控制与戒烟相关的体重增加；通过个体尝试戒烟来减少与戒烟相关的体重增加；治疗尼古丁依赖、成瘾和/或戒断的个体尝试治疗尼古丁依赖、成瘾和/或戒断；或减少个体尝试戒除尼古丁使用的复发可能性，包括给予选择性5-HT2C受体激动剂，可选地与辅助剂结合。