Development of Gastrointestinal Stimulants

At Ace Therapeutics, our team of scientists is deeply involved in investigating the complex mechanisms of various gastrointestinal diseases, and is committed to providing solutions for the study of various gastrointestinal diseases and advancing the development of therapeutic drugs for gastrointestinal diseases.

Introduction to Gastrointestinal Stimulants

Gastrointestinal stimulants are a class of drugs that promote gastric emptying and intestinal content transit by modulating the motor function of the gastrointestinal tract and are widely used in the treatment of diseases associated with gastrointestinal motility disorders.

• Functional Dyspepsia
• Gastroesophageal Reflux Disease (GERD)
• Stomach Cramps
• Irritable Bowel Syndrome (IBS)

Figure 1. Role of dietary manipulations and specific foods in functional dyspepsia pathophysiology. (Pesce M., et al. 2020)

Types of Gastrointestinal Stimulants We Can Develop

• Dopamine Receptor Antagonist
  Based on our clients' research and development needs, we develop dopamine receptor inhibitors and evaluate the efficacy of the drugs in relieving dopamine inhibition of the gastrointestinal tract, increasing lower esophageal sphincter pressure, decreasing gastroesophageal reflux and enhancing gastrointestinal motility.
• 5-Hydroxytryptamine (5-HT) Receptor Modulators
  We provide our clients with technical support and services for the development of 5-HT receptor modulators. For example, evaluating the efficacy of 5-HT receptor agonists in promoting the release of acetylcholine and enhancing the contraction of gastrointestinal smooth muscle and the ability of 5-HT receptor antagonists to attenuate nausea and vomiting while enhancing gastrointestinal motility.
• Cholinergic Receptor Agonist
  In the development process of cholinergic receptor antagonists, we provide clients with assistance in evaluating the ability of drug to directly activate cholinergic neurons, promote acetylcholine release, and enhance contraction of gastrointestinal smooth muscle.

What Can We Do for the Development of Gastrointestinal Stimulants?

In Vitro Studies

We support clients in studying the effects of gastrointestinal motility promoters on gastrointestinal smooth muscle motility and neural signaling with in vitro experiments in isolated intestinal smooth muscle, tissue slices, or cellular models.

• Smooth Muscle Contraction Assay
  Isolate intestinal segments from animals, place the segments in an organic bath maintained at physiological conditions of 37℃, add different concentrations of accelerators and record the strength and frequency of contraction of the muscle strips.
• Combined Neuromuscular Experiments
  Use intestinal segments containing enteric ganglia, add neurotransmitter antagonists or agonists, and observe changes in drug action to study the synergistic effects of facilitators on the enteric nervous system and muscle tissue.
• Receptor Binding Assay
  Test the affinity of a drug for a specific receptor and verify the relationship between the action of a facilitator and a specific receptor (such as 5-HT₄ receptor and dopamine D2 receptor) using radioactively or fluorescently labeled ligand binding assays.
• Ion Channel Modulation Experiments
  Add ion channel antagonists (like calcium channel blockers) to the intestinal smooth muscle to observe the changes in drug action and explore whether the drug affects the contraction of the gastrointestinal smooth muscle by modulating calcium or potassium channels.

In Vivo Studies

We also conduct in vivo experiments to observe the efficacy and mechanism of action of gastrointestinal peristalsis promoters by establishing animal models of gastrointestinal peristalsis dysfunction.

• Gastric Emptying Assay
  Assess the effect of drugs on the rate of emptying of gastric contents by giving animals semi-solid or liquid markers and taking samples over a fixed period of time.
• Intestinal Motility Measurement
  Use pressure transducers or myoelectric recording devices, we can measure the strength and frequency of peristaltic movements of the intestinal muscles and test the effect of drugs on the regulation of overall intestinal motility.

Based on our professional team of scientists and rich experience in research services, Ace Therapeutics is confident to help pharmaceutical companies and research organizations develop novel therapies for gastrointestinal diseases and to advance the research on gastrointestinal stimulants. If you are interested in our services, please do not hesitate to contact us.

Reference

1. Pesce, M.; et al. Diet and functional dyspepsia: Clinical correlates and therapeutic perspectives. World J Gastroenterol. 2020, 26(5):456-465.

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