Pirenzepine

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Pirenzepine
Clinical data
AHFS/Drugs.com Monograph
ATC code A02BX03 (WHO)
Identifiers
CAS Number 28797-61-7 YesY
PubChem (CID) 4848
IUPHAR/BPS 328
DrugBank DB00670 YesY
ChemSpider 4682 YesY
UNII 3G0285N20N YesY
KEGG D08389 YesY
ChEBI CHEBI:8247 YesY
ChEMBL CHEMBL9967 YesY
ECHA InfoCard 100.044.739
Chemical and physical data
Formula C19H21N5O2
Molar mass 351.403 g/mol
3D model (Jmol) Interactive image
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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 being 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. ↑ Stolerman, Ian P. (2 August 2010). Encyclopedia of Psychopharmacology. Springer. p. 811. ISBN 978-3-540-68698-9. Retrieved 26 June 2013.
  2. ↑ Czepita D (2005). "Fundamentals of modern treatment of myopia". Ann Acad Med Stetin. 51 (2): 5–9. PMID 16519089.
  3. ↑ Walline JJ, Lindsley K, Vedula SS, Cotter SA, Mutti DO, Twelker JD (2011). "Interventions to slow progression of myopia in children". Cochrane Database Syst Rev (12): CD004916. doi:10.1002/14651858.CD004916.pub3. PMC 4270373Freely accessible. PMID 22161388.
  4. ↑ Pediani JD, Ward RJ, Godin AG, Marsango S, Milligan G (2016): "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-Selective Antagonist Drugs." J Biol Chem. PMID 27080256


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