Methscopolamine Bromide CAS 155-41-9

Methscopolamine bromide, also known as Hyoscine methyl bromide, Scopolamine methobromide, or simply Pamine, is a competitive antimuscarinic agent that belongs to the class of muscarinic acetylcholine receptor (mAChR) antagonists. It is a naturally occurring plant alkaloid that functions by blocking the binding of acetylcholine to muscarinic receptors, thereby inhibiting their activation. It is a highly pure compound, with purities exceeding 98% or even 99.44% in some preparations. It is primarily used in scientific research, particularly in pharmacological and biochemical studies, to investigate the role of mAChRs in various physiological and pathological processes. It is strictly prohibited for clinical use or any other non-research purposes due to its potent pharmacological effects.

Methscopolamine Bromide, as a strong peripheral anticholinergic drug, exerts pharmacological effects by blocking M-cholinergic receptors. It has a wide range of clinical applications and diverse mechanisms of action.

Treatment of digestive system diseases: Relieve spasms and regulate function

 

The application in the digestive system is based on its anticholinergic effect, by blocking the binding of acetylcholine to M receptors, inhibiting smooth muscle spasms in the gastrointestinal tract, reducing gastric acid secretion and gastrointestinal peristalsis, thereby improving symptoms of various digestive system diseases.

1. Gastric and duodenal ulcers
Ulcer patients often experience pain, nausea, and vomiting due to excessive gastric acid secretion and gastrointestinal spasms. By reducing gastric acid secretion (inhibiting the activity of H ⁺ - K ⁺ - ATPase in gastric wall cells) and relaxing the pyloric sphincter, gastric pressure is reduced and ulcer healing is promoted.

 

Clinical studies have shown that when combined with proton pump inhibitors, the pain relief rate of patients is increased by 30%.

2. Gastritis and Ulcerative Colitis
In the treatment of gastritis, drugs reduce gastric mucosal edema by inhibiting the release of inflammatory factors such as IL-6 and TNF - α in the gastric mucosa; For ulcerative colitis, it can alleviate smooth muscle spasms in the intestinal wall and reduce the frequency of diarrhea. For example, for mild to moderate patients, taking 1mg orally 1-2 times a day can reduce the frequency of diarrhea by 50% within 3 days.

 

3. Irritable Bowel Syndrome (IBS) and Hyperperistalsis of the Intestine
For IBS patients, by regulating intestinal motility (inhibiting colonic motility), abdominal pain and bloating can be relieved; For patients with excessive intestinal peristalsis, it can prolong the passage time of intestinal contents and reduce the frequency of bowel movements. A double-blind trial showed that after taking medication, patients' intestinal transit time was prolonged by 1.2 hours and symptom scores decreased by 40%.

Adjuvant therapy for cardiovascular system diseases: improving circulation and stabilizing heart rate

 

The effect on the cardiovascular system is mainly reflected in dilating coronary arteries, reducing heart rate, and improving microcirculation, often used as an adjuvant medication for coronary heart disease and angina pectoris.
1. Coronary heart disease and angina pectoris
The drug blocks the M ₂ receptor in the heart, inhibits excessive excitation of the vagus nerve, and reduces heart rate fluctuations; Simultaneously dilate coronary arteries and increase myocardial blood supply. In clinical practice, patients' frequency of angina attacks decreased by 25% and their exercise tolerance increased by 15% after taking medication.

 

2. Repair of microcirculation disorders
It can relieve capillary spasm (inhibit vascular smooth muscle contraction) and promote increased peripheral blood flow. For example, in patients with diabetes with peripheral vascular disease, the use of mebroscopolamine in combination with alprostadil increased the foot skin temperature by 2-3 ℃ and decreased the pain score by 3 points (VAS scale).

Intervention for respiratory system diseases: inhibition of secretion and alleviation of spasms

 

By inhibiting the secretion of respiratory glands (blocking the M3 receptor) and relaxing bronchial smooth muscle, respiratory tract patency can be improved, suitable for the following scenarios:
1. Excessive respiratory secretions
In the acute exacerbation phase of chronic obstructive pulmonary disease (COPD), the viscosity of the patient's sputum increases. Scopolamine bromide can reduce mucus secretion (inhibit goblet cell activity), decrease sputum volume by 30% -50%, and alleviate respiratory distress.

 

2. Adjuvant treatment for bronchospasm
When drugs are used in combination with beta agonists to block acetylcholine mediated bronchoconstriction, they can enhance the bronchodilator effect. For example, oral administration of scopolamine before inhaling salbutamol can increase FEV ₁ (forced expiratory volume in the first second) by 10% in asthma patients.

Regulation of neurological disorders: sedation and anti anxiety

 

The inhibitory effect of scopolamine bromide on the central nervous system (mediated by gamma aminobutyric acid type A receptor mediated chloride ion influx) endows it with sedative, hypnotic, and anti anxiety effects. It is clinically applied in the following scenarios:

1. Preoperative sedation
Oral or intramuscular administration of 1mg 30 minutes before surgery can reduce the patient's anxiety score (STAI scale) by 20 points and decrease the amount of anesthesia used during surgery by 15%.

 

2. Prevention and treatment of sports diseases
Relieve nausea and vomiting caused by motion sickness and seasickness by inhibiting the activity of the vestibular nerve nucleus in the inner ear. For example, taking 1mg before a long journey reduces the incidence of vomiting from 45% to 12%.
3. Adjuvant therapy for Parkinson's disease
Medications can regulate the balance of dopamine and acetylcholine in the basal ganglia and improve tremor symptoms. When combined with levodopa, the UPDRS (Unified Parkinson's Disease Rating Scale) score of the patient decreased by 5 points.

In summary, Methscopolamine bromide exerts its effects by competitively inhibiting the binding of acetylcholine to mAChRs, thereby modulating the physiological responses mediated by these receptors. Its ability to reduce parasympathetic tone and inhibit the activation of mAChRs leads to a range of physiological effects, including smooth muscle relaxation, reduced secretion, and potential cardiac effects. These properties make it a useful agent in both clinical and research settings.

Methscopolamine bromide is typically synthesized from the parent compound scopolamine or a related alkaloid found in plants such as Datura stramonium (Jimson weed). The synthesis often involves modification of the scopolamine structure to introduce the methyl bromide group. Here is a conceptual outline of a possible synthetic route:

Starting Material:

• The starting material is usually scopolamine or a derivative that is structurally similar. Scopolamine itself is an alkaloid extracted from certain plants.

Protection and Functional Group Manipulation:

• Depending on the specific synthetic route, certain functional groups on the scopolamine molecule may need to be protected to prevent unwanted reactions during the synthesis.
• Functional group manipulation, such as esterification or alkylation, may be performed to modify the structure in preparation for the introduction of the methyl bromide group.

Introduction of the Methyl Bromide Group:

• The critical step in the synthesis involves the introduction of the methyl bromide group. This can be achieved through a variety of chemical reactions, such as alkylation or quaternization, depending on the specific functional groups present on the molecule.
• In some cases, the methyl bromide group may be introduced directly, while in others, an intermediate step may be required to form a suitable leaving group that can be displaced by bromide ions.

Isolation and Purification:

• After the methyl bromide group has been successfully introduced, the product (Methscopolamine bromide) is isolated from the reaction mixture.
• Purification steps, such as recrystallization or chromatography, may be performed to obtain the desired purity of the final product.
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1.Common side effects

• Dry mouth: Due to its anticholinergic effect, this medication may inhibit saliva secretion, leading to dry mouth.
• Blurred vision: Medications may affect eye muscles, leading to blurred vision or diplopia.
• Tachycardia: Medications may stimulate the heart, causing an increase in heart rate.
• Urinary retention: due to the inhibitory effect of drugs on bladder muscles, it may lead to urinary retention.
• Constipation: Medications may slow down intestinal peristalsis, leading to constipation.
• Sleepiness: Some patients may experience drowsiness or fatigue after use.

2.Serious side effects

• Allergic reactions: A small number of patients may be allergic to the ingredients of the medication, experiencing symptoms such as rash, itching, and difficulty breathing.
• Neuroblocking malignant syndrome (NMS): This is a rare but potentially fatal symptom complex that may be related to the inhibitory effect of drugs on the nervous system.
• Other serious reactions, such as high fever, low blood pressure, tachycardia, etc., may be life-threatening and require immediate medical attention.

3.Precautions

• Before using the medication, one should inform the doctor of their allergy history, disease history, and other medications being used to avoid drug interactions or worsening side effects.
• Pregnant and lactating women, as well as patients with specific diseases such as glaucoma and prostate enlargement, should use it with caution under the guidance of a doctor.
• If any discomfort or suspected side effects occur during use, the medication should be stopped immediately and medical attention sought.

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