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Systematic (IUPAC) name
Clinical data
AHFS/Drugs.com Monograph
CAS Number 28797-61-7 YesY
ATC code A02BX03 (WHO)
PubChem CID 4848
DrugBank DB00670 YesY
ChemSpider 4682 YesY
UNII 3G0285N20N YesY
KEGG D08389 YesY
Chemical data
Formula C19H21N5O2
Molar mass 351.403 g/mol

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[edit]


  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 4270373free to read. 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