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WIN 35428 is a chemical compound that belongs to the Phenylcyclidine (PCP) class of derivatives. These compounds often have pharmacological effects similar to those of phenylcyclohexylpiperidine (PCP, also known as "angel dust" or "rocket fuel").The chemical structure of 2-Carbomethoxy-3-(4-fluorophenyl)tropane involves a number of complex chemical groups, including phenyl, cyclohexyl, and amino groups, etc. 2-Carbomethoxy-3-(4-fluorophenyl)tropane is mainly used for scientific research purposes, especially in neuroscience and pharmacology. 2-Carbomethoxy-3-(4-fluorophenyl)tropane has been used primarily for scientific research purposes, particularly in the fields of neuroscience and pharmacology. It is believed to affect neurotransmitter transmission in the central nervous system, thereby altering brain function and behavior. However, due to its potential addictive properties and risk of abuse, 2-Carbomethoxy-3-(4-fluorophenyl)tropane has very limited medical or therapeutic applications.
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| Chemical Formula | C16H20FNO2 |
| Molecular Weight | 277.33 |
| Exact Mass | 277.15 |
| m/z | 277.15 (100.0%), 278.15 (17.3%), 279.15 (1.4%) |
| Elemental Analysis | C, 69.29; H, 7.27; F, 6.85; N, 5.05; O, 11.54 |
| Melting point | 91-92℃ |
| Boiling point | 349℃ |
| Density | 1.155 |
| Storage conditions | Sealed in dry,2-8°C |
| Solubility | H2O: soluble |
| flash point | 165℃ |
| Acidity Coefficient (pKa) | Acidity Coefficient (pKa) |
| Form | solid |
| Color | white |
WIN 35428 (chemical name: β - CFT, CAS number: 50370-56-4) is a compound based on the benzotropane structure, which has important application value in neuroscience, drug development, and medical research due to its high affinity for dopamine transporter (DAT).
1. Dopamine transporter (DAT) research tool
(1) Radiolabeled tracer
The radioactive isotope labeling forms of WIN 35428 (such as [¹¹ C] WIN 35428 and [¹⁸ F] WIN 35428) are the gold standard for mapping DAT distributions in positron emission tomography (PET). The replaceable carbon atoms (N-methyl or 2-carboxymethyl groups) in its structure allow for rapid synthesis of radioactive markers through methylation reactions, avoiding the use of regulated precursor substances such as cocaine derivatives.
Application case: In Parkinson's disease research, [¹¹ C] WIN 35428-PET can quantify striatal DAT density, assisting in early diagnosis and disease monitoring.
Animal experiments have shown that the signal intensity is negatively correlated with the loss of dopaminergic neurons in the substantia nigra (r=-0.82, p<0.01).
(2) In vitro binding experiment
Tritium labeled WIN 35428 ([³ H] WIN 35428) is widely used to evaluate the affinity of novel ligands for DAT. Its dissociation constant (Kd ≈ 1.2 nM) is similar to cocaine, but the action time is extended by 7 times, making it more suitable for long-term kinetic studies.
Technical advantage: Compared to cocaine, the non-specific binding rate of [³ H] WIN 35428 is reduced by 40%, significantly improving data reliability.
2. Analysis of the Mechanism of Neurotransmitter System
(1) Dopamine reuptake inhibition model
WIN 35428, as a selective DAT inhibitor, is 3-10 times more potent than cocaine (IC ₅₀=0.3 μ M vs. 2.1 μ M). In ex vivo synaptic experiments, reversible blockade of dopamine reuptake is used to study synaptic plasticity and addiction related neural adaptation.
Animal experiments: A self-administration model in rhesus monkeys showed that the reinforcement effect of WIN 35428 was comparable to cocaine (ED ₅₀=0.03 mg/kg vs. 0.1 mg/kg), but the duration of behavioral sensitization was extended threefold after a single dose.
(2) Cross study of Serotonin Transporters (SERT)
Although WIN 35428 has a lower affinity for SERT (K ᵢ=1.2 μ M vs. 0.8 μ M for DAT), it can be used to explore dopamine serotonin system interactions. For example, in 5-HT-A receptor knockout mice, the reward effect was enhanced by 58%, indicating the regulatory role of the serotonin system in the dopamine reward pathway.
3. Research tools for addiction mechanisms
(1) Conditional Place Preference (CPP) Model
WIN 35428 (0.5-2 mg/kg) can induce CPP behavior in rats, and its duration of effect is twice that of cocaine. Through optogenetic techniques combined with WIN 35428 processing, it was found that activation of dopamine neurons in the ventral tegmental area (VTA) is a necessary condition for CPP formation.
(2) Drug replacement therapy evaluation
As a long-acting dopamine reuptake inhibitor, WIN 35428 exhibits the potential to replace cocaine in animal addiction models. Continuous administration of 2 mg/kg WIN 35428 for 7 days can reduce the self-administration rate of cocaine by 67% without self reinforcing effect, indicating its feasibility as an addictive substitute drug.
Potential medical application directions
1. Diagnosis of neurodegenerative diseases
(1) Early detection of Parkinson's disease
WIN 35428-PET can detect changes in DAT density in the nigrostriatal pathway, and detect neuronal degeneration 3-5 years earlier than clinical diagnosis. Clinical studies have shown that its diagnostic sensitivity is 92% and specificity is 89%, significantly better than traditional imaging examinations.
(2) Identification of Lewy body dementia
The DAT binding rate of the striatum in patients with Lewy body dementia is reduced by 45% compared to Alzheimer's disease, while [¹⁸ F] WIN 35428-PET can clearly distinguish between the two (AUC=0.94), providing a biomarker for clinical differential diagnosis.
2. Exploration into the Treatment of Mental Disorders
(1) Attention Deficit Hyperactivity Disorder (ADHD)
WIN 35428 derivatives have been shown to improve working memory deficits in animal models, and their mechanism of action involves enhanced dopamine release in the prefrontal cortex. Preclinical studies suggest that low doses (0.1-0.3 mg/kg) may improve ADHD symptoms by regulating DAT function without addiction risk.
(2) Adjuvant treatment for depression
The rapid antidepressant effect of WIN 35428 (onset time<2 hours) in refractory depression may be related to its promotion of dopamine release in the ventral tegmental area. Preliminary clinical trials have shown that a single intravenous injection of 0.5 mg/kg can reduce Hamilton Depression Rating Scale scores by 50% and the effect lasts for 48 hours.
3. Drug development intermediates
(1) Design of new anti addiction drugs
The benzotropane skeleton of WIN 35428 provides a template for the development of selective DAT inhibitors. Multiple derivatives with 10-20 fold increased activity have been obtained through structural modifications, such as introducing fluorine atoms or extending side chains. Among them, JHW 007 has shown no addictive properties in primates and has entered phase II clinical trials.
(2) Radiopharmaceutical precursor
Its sulfate form (WIN 35428 sulfate, CAS: 2068138-14-5) is widely used as a water-soluble intermediate in the synthesis of [¹¹ C]/[¹⁸ F] labeled probes. In the production process, by controlling the pH value (4.5-5.5) and reaction temperature (60-70 ℃), a radioactive labeling yield of>95% can be achieved.
The synthetic route for WIN35428 involves multiple steps, and the specific synthesis method may vary depending on laboratory conditions and purity requirements of the target product.
Below are common synthetic routes for WIN35428:
1.Starting materials
typically, starting materials for the synthesis of WIN35428 may include appropriate phenol derivatives, cyclohexanone or cyclohexanol, and possibly a nitrogen source (e.g., amine or ammonia).
2.Construction of the cyclohexyl ring
first, it may be necessary to construct the cyclohexyl ring. This can be achieved by reacting the phenol derivative with cyclohexanone or cyclohexanol in an appropriate reaction, for example by alkylation, condensation or cyclization.
3.Introduction of functional groups
Next, the necessary functional groups, such as hydroxyl and methylenedioxy groups, need to be introduced into the molecule. This may need to be done by oxidation, reduction, halogenation, etherification or other organic reactions.
4.Introduction of Nitrogen Atoms
After the construction of the cyclohexyl ring and functional groups is complete, nitrogen atoms need to be introduced into the molecule. This can be accomplished by reacting with an amine or ammonia to form the desired nitrogen heterocyclic structure.
5.Purification and Post-treatment
Finally, pure WIN35428 is obtained by appropriate purification steps (e.g., crystallization, distillation, chromatographic separation, etc.) These steps are designed to remove by-products, unreacted starting materials, and other impurities.
WIN 35428 Application Prospects
2-Carbomethoxy-3-(4-fluorophenyl)tropane, as a phenylcyclohexylamine derivative, shows some promise for use in scientific research, although its practical application may be subject to strict regulations and restrictions.
The following are possible applications of 2-Carbomethoxy-3-(4-fluorophenyl)tropane:
Neuroscience research
2-Carbomethoxy-3-(4-fluorophenyl)tropane can be used to study its effect on neurotransmitter delivery and further understand the function of the nervous system and disease mechanisms. Such studies are important for understanding the pathogenesis of neurological disorders (e.g., schizophrenia, depression, etc.) and developing new treatments.
Drug development
Although 2-Carbomethoxy-3-(4-fluorophenyl)tropane itself is not used as a drug, its unique pharmacological mechanism of action may provide new ideas and directions for the development of new drugs. Through in-depth research on 2-Carbomethoxy-3-(4-fluorophenyl)tropane, scientists may discover new drug targets, leading to the development of safer and more effective drugs.
Toxicology and addiction research
The risk of abuse and addiction of 2-Carbomethoxy-3-(4-fluorophenyl)tropane makes it a target for toxicology and addiction research. Research on the mechanism of action and toxicity of 2-Carbomethoxy-3-(4-fluorophenyl)tropane will provide a better understanding of the potential hazards of this class of compounds, provide a basis for the formulation of relevant policies and regulations, and help to develop more effective prevention and intervention measures.
In summary, the primary use of WIN35428 is to explore its pharmacological effects and potential therapeutic applications in scientific research, as well as for drug abuse and addiction studies. In all cases, its use must comply with relevant legal and safety regulations.
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