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general/4-methylpiperazin-1-yl-compounds

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Pirenzepine

Chemical compound

Summary

Chemical compound

| Drugs.com =

Pirenzepine (Gastrozepin), an M1 selective antagonist, is used in the treatment of peptic ulcers, as it reduces gastric acid secretion and reduces muscle spasm. It is in a class of drugs known as muscarinic receptor antagonists; acetylcholine is the neurotransmitter of the parasympathetic nervous system which initiates the rest-and-digest state (as opposed to fight-or-flight), resulting in an increase in gastric motility and digestion; whereas pirenzepine would inhibit these actions and cause decreased gastric motility leading to delayed gastric emptying and constipation. It has no effects on the brain and spinal cord as it cannot diffuse through the blood–brain barrier.

Pirenzepine has been investigated for use in myopia control.

It promotes the homodimerization or oligomerisation of M1 receptors.

References

References

  1. (2 August 2010). "Encyclopedia of Psychopharmacology". Springer.
  2. (2005). "[Fundamentals of modern treatment of myopia]". Annales Academiae Medicae Stetinensis.
  3. (January 2020). "Interventions to slow progression of myopia in children". The Cochrane Database of Systematic Reviews.
  4. (June 2016). "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs". The Journal of Biological Chemistry.
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4-methylpiperazin-1-yl-compounds acetamides lactams m1-receptor-antagonists m4-receptor-antagonists peripherally-selective-drugs pyridobenzodiazepines
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