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Clinical data
AHFS/Drugs.com Monograph
ATC code
CAS Number
PubChem CID
ECHA InfoCard 100.044.739
Chemical and physical data
Formula C19H21N5O2
Molar mass 351.403 g/mol
3D model (JSmol)

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 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