Chemistry:Pirenzepine

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Short description: Chemical compound
Pirenzepine
Pirenzepine.png
Clinical data
Trade namesGastrozepin
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC19H21N5O2
Molar mass351.410 g·mol−1
3D model (JSmol)
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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.[1] 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.[2][3]

It promotes the homodimerization or oligomerisation of M1 receptors.[4]

See also

References

  1. Encyclopedia of Psychopharmacology. Springer. 2 August 2010. p. 811. ISBN 978-3-540-68698-9. https://books.google.com/books?id=qoyYobgX0uwC&pg=PA811. Retrieved 26 June 2013. 
  2. "[Fundamentals of modern treatment of myopia]". Annales Academiae Medicae Stetinensis 51 (2): 5–9. 2005. PMID 16519089. 
  3. "Interventions to slow progression of myopia in children". The Cochrane Database of Systematic Reviews 1 (1): CD004916. January 2020. doi:10.1002/14651858.CD004916.pub4. PMID 31930781. 
  4. "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs". The Journal of Biological Chemistry 291 (25): 13132–13146. June 2016. doi:10.1074/jbc.M115.712562. PMID 27080256.