Ace Therapeutics
Development of Antispasmodics for Gastrointestinal Diseases
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Development of Antispasmodics for Gastrointestinal Diseases

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Ace Therapeutics is committed to supporting our partners in the development of antispasmodics for the treatment of gastrointestinal (GI) diseases. We have extensive experience in the development of agents targeting pathways involved in GI motility. Our customized disease models aid in assessing mechanisms of action, efficacy in lowering luminal pressure/intestinal contractions, and tolerability of drug candidates.

Introduction to Gastrointestinal Spasms

Spasms of the gastrointestinal tract are involuntary contractions of the muscles in the digestive tract that often cause pain, cramping, and discomfort. These spasms can occur in various parts of the digestive system, from the esophagus to the colon, and are often associated with diseases such as irritable bowel syndrome (IBS), gastritis, and dyspepsia. Antispasmodic drugs, such as hyoscyamine and dicyclomine, which relax the smooth muscles of the gut, are commonly used to reduce muscle spasms. Additionally, a combination of medications such as anticholinergics and calcium channel blockers may be used to relieve severe symptoms.

Figure 1. Effect of PPIs on gastric physiologyFigure 1. Essential oils and their antispasmodic mechanisms on the abdominal organs. (Heghes S.C., et al., 2019)

Types of Antispasmodics We Can Develop

  • Muscarinic Antagonists

We can assist customers in developing muscarinic antagonists that block the action of acetylcholine at muscarinic receptors, thereby reducing muscle contractions in the gastrointestinal tract. Our services include formulation, optimization, and efficacy testing of agents such as hyoscine and dicyclomine.

  • Calcium Channel Blockers

We specialize in the development of calcium channel blockers targeting voltage-gated calcium channels involved in smooth muscle contraction. Our services encompass lead optimization to enhance the potency and selectivity of candidates. We also provide in vivo models to assess the efficacy of compounds in reducing gastrointestinal spasms and improving gut motility and function.

  • Direct Smooth Muscle Relaxants

Our expertise extends to the development of direct smooth muscle relaxants that act on the intracellular signaling pathways involved in muscle contraction. We can conduct in vitro and in vivo studies to assess the efficacy of direct smooth muscle relaxants in reducing gastrointestinal spasms and improving gut motility.

What We Can Do for the Development of Antispasmodics?

In VitroStudies In Vivo Studies
  • Organ Bath Studies: Measure changes in muscle tension in response to antispasmodic agents using smooth muscle strips isolated from animal models.
  • Calcium Imaging Assays: Monitor intracellular calcium levels in smooth muscle cells to assess the effect of antispasmodics on calcium signaling.

We can construct animal models of gastrointestinal diseases according to your needs.

  • Irritable Bowel Syndrome (IBS) Models: Assess the efficacy of antispasmodics in reducing abdominal pain and discomfort.
  • Models of Gastritis or Dyspepsia: Evaluate the ability of antispasmodics to alleviate symptoms associated with stomach spasm.

We evaluate the efficacy of antispasmodics by the following parameters and studies.

  • Behavioral Studies: Observe and record changes in animal behavior in response to treatment.
  • Pharmacodynamic Studies: Analysis of drug levels in blood and tissues over time and correlation of drug concentration with pharmacological effect.
  • Histological Analysis: Exanmine the expression of relevant proteins and morphological changes using immunohistochemical methods.
  • Electrophysiological Studies: Record electrical activity in smooth muscle tissues and analyze changes in electrophysiological properties in response to antispasmodic treatment.

By providing comprehensive in vitro and in vivo evaluation services, Ace Therapeutics empowers pharmaceutical companies and research institutions to develop novel therapies for spasms of the gastrointestinal tract. Contact us today to discuss your specific needs and receive a customized quote.

References

  1. Heghes S.C., et al. Antispasmodic effect of essential oils and their constituents: A review. Molecules. 2019, 24(9):1675.
  2. Annaházi A., et al. Role of antispasmodics in the treatment of irritable bowel syndrome. World J Gastroenterol. 2014, 20(20):6031-43.

Our products and services are for research use only and can not be used for diagnostic or other purposes.