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Scopolamine hydrobromide powder is a pharmaceutical grade compound belonging to the tropane alkaloid family, derived from the nightshade plant genus Solanum or Datura. It is a white to off-white, crystalline powder, highly soluble in water and alcohol, making it a versatile formulation for medical use. Primarily known for its anticholinergic and sedative properties, Tranaxine acts on the central nervous system (CNS) to disrupt the normal functioning of acetylcholine, a neurotransmitter crucial for numerous bodily functions including memory, learning, and muscle control.
In therapeutic applications, it's most commonly used as a pre-anesthetic medication to reduce anxiety and secretions in the respiratory tract prior to surgery. It can also alleviate nausea and vomiting associated with motion sickness, postoperative recovery, or certain medical conditions like chemotherapy. However, due to its potential for side effects such as drowsiness, blurred vision, and memory loss (particularly "dry mouth" or anticholinergic syndrome), its use is strictly controlled and prescribed by healthcare professionals.
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Chemical Formula |
C17H22BrNO4 |
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Exact Mass |
383.07 |
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Molecular Weight |
384.27 |
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m/z |
383.07 (100.0%), 385.07 (97.3%), 386.07 (17.9%), 384.08 (16.2%), 384.08 (2.2%), 387.08 (1.2%), 385.08 (1.1%) |
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Elemental Analysis |
C, 53.14; H, 5.77; Br, 20.79; N, 3.65; O, 16.65 |
synthesis methods
Trost synthesis method
Scopolamine hydrobromide powder is a type of tropane alkaloid, and its synthesis typically involves complex organic chemical reactions, particularly the construction of chiral centers and the transformation of functional groups.
Regarding the mention of the "Trost synthesis method", although it is not directly used for the synthesis of tranaxine, Professor Trost and his team's contributions in the field of asymmetric catalysis have provided the possibility for efficient and highly selective synthesis of many complex organic molecules.
Selection of starting materials and preliminary conversion
- Usually, it does not start directly from dichloromethane, but from aromatic compounds containing appropriate functional groups. For example, benzene ring compounds containing easily convertible methyl or halogen substituents can be used.
- Perform Friedel Crafts acylation or alkylation reactions, introduce specific side chains or functional groups, and lay the foundation for subsequent synthesis steps.
Constructing the backbone of tropane
- This step is the core of synthesizing scopolamine and its analogues, usually involving multiple reactions including cyclization, reduction, functional group conversion, etc.
- The basic skeleton of tropane may be constructed from aromatic compounds or other intermediates through a series of reactions such as cycloaddition, oxidation, reduction, etc.
Fine adjustment of functional groups
- After obtaining the backbone of tropane, it is necessary to further fine tune its functional groups to meet the structural requirements of scopolamine.
- This may include reactions such as esterification, acylation, amination, halogenation, as well as possible chiral center construction or maintenance.
Final conversion and purification
- After the above steps, the obtained compound needs to be converted into tranaxine.
- This may involve a reaction with hydrobromic acid to introduce bromide ions and simultaneously form salts.
- Finally, high-purity tranaxine is obtained through appropriate purification methods such as recrystallization, chromatographic separation, etc.
Robinson synthesis method
Normally, morphine is not directly used as a starting material because there is a significant difference in chemical structure between scopolamine and morphine. The more common starting materials may be precursors of tropinone or other related alkaloids.
By oxidation, reduction, cyclization and other reactions, the starting materials are converted into compounds containing a tropane skeleton.
Introduce necessary functional groups such as hydroxyl, ester, and amine groups onto the backbone of tropane to meet the structural requirements of scopolamine.
These steps may involve multi-step reactions such as acylation, alkylation, oxidation, etc.
Scopolamine is a compound with a chiral center, so special attention should be paid to the construction and maintenance of the chiral center during the synthesis process.
Advanced technologies such as asymmetric catalysis may be required to achieve highly selective synthesis.
After the above steps, the obtained compound needs to be further converted into scopolamine.
Finally, it reacts with hydrobromic acid to produce tranaxine.
High purity tranaxine can be obtained through appropriate purification methods such as recrystallization, chromatographic separation, etc
muscarinic receptors
Muscarinic receptors are a class of G protein-coupled receptors (GPCRs) that play a pivotal role in mediating the actions of the neurotransmitter acetylcholine (ACh) in both the central nervous system (CNS) and the peripheral nervous system (PNS). They are named after the alkaloid muscarine, a naturally occurring compound that mimics the effects of ACh on these receptors.
There are five major subtypes of muscarinic receptors, designated as M1 to M5, each with distinct tissue distributions and functional roles. M1 receptors are primarily found in the CNS, particularly in the cortex and hippocampus, where they regulate cognitive processes, arousal, and memory. M2 receptors are abundant in the heart, where they inhibit heart rate and contractility, and in the CNS, where they modulate neurotransmitter release.
M3 receptors are predominantly expressed in smooth muscle tissues, such as those found in the bladder, gut, and airways, mediating contraction and secretory responses. M4 receptors are also present in the CNS, involved in modulating neurotransmitter release and contributing to cognitive function. Lastly, M5 receptors are less well-understood but are thought to be involved in the regulation of lipid metabolism and insulin secretion.
Dysregulation of muscarinic receptor signaling has been implicated in various disorders, including Alzheimer's disease, Parkinson's disease, schizophrenia, and certain cardiovascular conditions. Consequently, muscarinic receptor antagonists and agonists are important therapeutic targets for the treatment of these conditions, offering a means to modulate the body's response to ACh and restore balance to critical physiological processes.
Scopolamine hydrobromide is an anticholinergic drug that exerts a wide range of pharmacological effects by blocking M-cholinergic receptors, and its uses cover multiple clinical fields.
Core therapeutic areas: smooth muscle spasm and glandular secretion inhibition
Smooth muscle spasm related diseases
Gastrointestinal colic: By blocking the M-cholinergic receptors in the smooth muscles of the gastrointestinal tract, the excitatory effect of acetylcholine is reduced, and spastic pain is relieved. Commonly used for abdominal pain caused by irritable bowel syndrome, postoperative intestinal bloating, etc.
Gallbladder and renal colic: Relieve smooth muscle spasms in the biliary and urinary tract, and alleviate pain caused by cholecystitis, gallstones, or kidney stones.
Bronchial spasm: dilates the bronchi and assists in the treatment of acute asthma attacks or acute exacerbations of chronic obstructive pulmonary disease (COPD).
Glandular secretion inhibition
Pre anesthesia administration: Reduce the secretion of salivary glands, bronchial glands, and sweat glands to prevent aspiration and airway obstruction during anesthesia induction.
Salivation: Control excessive saliva caused by Parkinson's disease or drug side effects, and improve the quality of life of patients.
Hyperhidrosis: Inhibits sweat gland secretion and alleviates local or systemic hyperhidrosis.
Special symptom treatment: central and peripheral synergistic effects
Motion sickness (motion sickness, seasickness, airsickness)
Mechanism: By inhibiting the excitability of the vestibular nucleus and cerebellar reticular formation, it reduces nausea and vomiting caused by excessive stimulation of the vestibular organs in the inner ear.
Usage: Oral tablets or transdermal patches (such as compound hydrobromic acid scopolamine patch) should be applied to the hairless area behind the ear 4 hours before driving, and the effect can last for 12-72 hours.
Advantages: Combined use with diphenhydramine can enhance therapeutic efficacy, and transdermal patches avoid the first pass effect of oral administration.
Tremor paralysis (Parkinson's disease)
Mechanism: As a central anticholinergic drug, it regulates the balance of dopamine and acetylcholine in the substantia nigra striata pathway, improving resting tremor and muscle rigidity.
Attention: It should be used in combination with levodopa, as its effectiveness is limited when used alone and may induce psychiatric symptoms.
Manic psychosis
Mechanism: Relieve excitement, aggressive behavior, and sleep disorders during manic episodes through central inhibitory effects.
Limitations: Currently, it is not a first-line medication and is mostly used for adjuvant therapy or for patients who are intolerant to other drugs.
First aid and poisoning treatment: life support and detoxification
Septic shock
Mechanism: Expand peripheral blood vessels, increase blood flow, improve microcirculation, while stimulating the respiratory center and enhancing tissue oxygen supply.
Usage: Intravenous injection, blood pressure and heart rate should be monitored to avoid excessive cardiac arrhythmia.
Organophosphorus pesticide poisoning
Mechanism: As an anticholinergic drug, it combats muscarinic symptoms such as pupil constriction, bronchospasm, salivation, and diarrhea.
Usage: Used in combination with acetylcholinesterase activators (such as chlorpromazine), administered intravenously, with the dosage adjusted according to the degree of toxicity until reaching "atropine like" (dry mouth, dry skin, increased heart rate).
Attention: Close observation of the condition is necessary to avoid excessive central excitation (delirium, convulsions) or respiratory depression.
Ophthalmic applications: local treatment and contraindications
Iridocyclitis
Mechanism: Local eye drops can dilate the pupils, prevent posterior adhesion of the iris, and alleviate inflammatory reactions.
Usage: 1-2 times a day, with dilated pupils lasting for 7-10 days, during which strong light stimulation should be avoided.
Taboo: Not recommended for patients with angle stenosis or glaucoma, as it may trigger acute angle closure glaucoma attacks.
Other uses: Interdisciplinary exploration
Preoperative preparation for endoscopic examination
Purpose: To reduce gastrointestinal peristalsis and facilitate gastroscopy, colonoscopy, or ERCP (endoscopic retrograde cholangiopancreatography) procedures.
Advantages: Combined use with antispasmodics such as scopolamine can enhance the effect.
postoperative ileus
Mechanism: Promote the recovery of gastrointestinal peristalsis and shorten the time for intestinal function recovery.
Attention: Use only after ruling out mechanical obstruction.
structural characteristics
- Van der Waals force interaction
The benzene ring and five membered heterocyclic ring in scopolamine hydrobromide powder both have semi polarity, resulting in van der Waals force interactions with surrounding molecules, forming intermolecular attraction.
- Ester bond
The carboxylic acid groups in tranaxine molecules undergo esterification reaction with ethanol molecules, forming ester bonds. The formation of this ester bond, to a certain extent, increases the chemical stability of tranaxine molecule.
- Pyridine heterocycles
The center of the tranaxine molecule is a nitrogen-containing six membered heterocycle (pyridine ring). There is also a carboxylic acid group and a methoxy group on the pyridine ring, which are key parts of its anticholinergic effect.
- Quad Ring
The tranaxine molecule contains a quaternary ring structure that can be associated with the μ Type I opioid receptors bind to exert anti anesthetic effects.
- Hydroxy and methoxy groups
Tranaxine molecules also contain multiple hydroxyl and methoxy groups. These functional groups have certain hydrolytic properties and can combine with cholinesterase to produce anticholinergic effect.
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