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Acotiamide

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Acotiamide

acotiamide

Acotiamide is primarily associated with the management and research of functional dyspepsia and gastric motility disorders, particularly conditions involving impaired gastric accommodation, delayed gastric emptying, and postprandial gastrointestinal symptoms.

Chemical Information:

  • Product Name: Acotiamide
  • CAS No.: 185106-16-5
  • Molecular Formula: C₂₁H₃₀N₄O₅S
  • Molecular Weight: 450.55 g/mol
  • Chemical Class: Salicylamide derivative
  • Category: Gastrointestinal Prokinetic Agent
  • Form: Solid / powder
  • Synonyms: Z-338, YM-443, Acotiamide free base

Description:

Acotiamide is a gastrointestinal prokinetic agent that enhances upper gastrointestinal motility and supports gastric emptying. It is a selective and reversible acetylcholinesterase (AChE) inhibitor and also acts on presynaptic muscarinic pathways involved in acetylcholine release. These combined pharmacological actions increase cholinergic activity in the gastrointestinal tract and can improve gastric contractility and motility.

Applications

Acotiamide is used in pharmaceutical research and development as a gastrointestinal motility-modulating compound.

Key Applications

  • Functional Dyspepsia Research: Investigated for symptoms associated with impaired gastric motility and delayed gastric emptying.
  • Gastrointestinal Motility Studies: Used to investigate mechanisms regulating gastric contractility and upper GI transit.
  • Gastric Emptying Research: Studied for its ability to enhance gastric contractility and accelerate delayed gastric emptying.
  • Prokinetic Drug Development: Used as a reference or active pharmaceutical ingredient in research involving gastrointestinal prokinetic therapies.
  • Pharmacological Research: Useful for investigating acetylcholinesterase inhibition and cholinergic regulation of gastrointestinal function.

Acotiamide has been clinically developed for functional dyspepsia and is marketed as acotiamide hydrochloride hydrate in Japan.

Product Specifications

Acotiamide should be handled in accordance with the applicable Safety Data Sheet (SDS) and site-specific chemical handling procedures.

Handling Precautions

  • Avoid unnecessary generation and inhalation of dust.
  • Avoid direct contact with eyes, skin and clothing.
  • Use appropriate personal protective equipment (PPE), including gloves and safety eyewear.
  • Handle in a well-ventilated area or under suitable local exhaust ventilation.
  • Wash hands thoroughly after handling.
  • Avoid eating, drinking or smoking while handling the material.
  • Keep the container tightly closed when not in use.

Laboratory / Research Use

For laboratory and pharmaceutical development applications, appropriate containment and handling procedures should be followed. Acotiamide should not be administered to humans or animals solely on the basis of research-grade material specifications.

For pharmaceutical use, always follow the applicable regulatory requirements, approved product information, SDS and qualified medical/pharmaceutical guidance.

Mechanism of Actions

Acotiamide produces its gastroprokinetic effects through cholinergic mechanisms in the gastrointestinal tract.

1. Acetylcholinesterase Inhibition

Acotiamide selectively and reversibly inhibits acetylcholinesterase (AChE), reducing the breakdown of acetylcholine. This increases the availability of acetylcholine at cholinergic nerve terminals and enhances gastrointestinal motor activity.

2. Muscarinic M1/M2 Modulation

Acotiamide also acts on presynaptic M1 and M2 muscarinic receptors, helping enhance acetylcholine release from enteric cholinergic neurons.

3. Enhanced Gastric Motility

The resulting increase in cholinergic signaling can enhance gastric contractility and facilitate gastric emptying, supporting its prokinetic activity.

Simplified pathway:

Acotiamide → AChE inhibition + presynaptic M1/M2 modulation → increased acetylcholine availability/release → enhanced gastric motor activity → improved gastric emptying

FAQs

1. What is Acotiamide?

Acotiamide is a gastrointestinal prokinetic agent that enhances GI motility through cholinergic mechanisms, including selective and reversible inhibition of acetylcholinesterase.

2. What is the CAS number of Acotiamide?

The CAS number of Acotiamide free base is 185106-16-5.

3. What is the molecular formula of Acotiamide?

The molecular formula is C₂₁H₃₀N₄O₅S.

4. What is the molecular weight of Acotiamide?

The molecular weight of Acotiamide is approximately 450.55 g/mol.

5. What is Acotiamide used for?

Acotiamide is primarily associated with gastrointestinal motility and functional dyspepsia research, including studies involving delayed gastric emptying and impaired gastric motor function.

6. How does Acotiamide work?

It primarily enhances cholinergic activity by inhibiting acetylcholinesterase and modulating presynaptic muscarinic M1/M2 receptors, increasing acetylcholine availability and promoting gastrointestinal motor activity.

7. Is Acotiamide the same as Acotiamide Hydrochloride?

No. Acotiamide free base (CAS 185106-16-5) and Acotiamide hydrochloride/hydrate are different chemical forms. Acotiamide hydrochloride trihydrate is listed separately with CAS 773092-05-0 and a molecular weight of approximately 541.1 g/mol.

8. How should Acotiamide be stored?

For research-grade material, long-term powder storage is commonly specified at −20°C, protected from moisture and light. Always prioritize the storage conditions stated on the specific product’s COA/SDS.

9. Is Acotiamide soluble in water?

Acotiamide free base has very limited water solubility; published supplier data report it as insoluble or practically insoluble in water, while solubility can be substantially higher in certain organic solvents.

10. Is Acotiamide suitable for pharmaceutical manufacturing?

Acotiamide is a pharmacologically active compound used in pharmaceutical development. Whether a particular material is suitable for pharmaceutical manufacturing depends on its grade, manufacturing controls, regulatory status, analytical specifications, GMP documentation and batch-specific quality documentation.

11. What documentation can be provided with Acotiamide?

Depending on the grade and supplier, documentation may include a Certificate of Analysis (COA), Safety Data Sheet (SDS), specification sheet, analytical data and other quality/regulatory documents.

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