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Pirenzepine Trade names Gastrozepin AHFS /Drugs.com International Drug Names ATC code
11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H -pyrido[2,3-b ][1,4]benzodiazepin-6-one
CAS Number PubChem CID IUPHAR/BPS DrugBank ChemSpider UNII KEGG ChEBI ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.044.739 Formula C 19 H 21 N 5 O 2 Molar mass 351.410 g·mol−1 3D model (JSmol )
O=C3c1ccccc1N(C(=O)CN2CCN(C)CC2)c4ncccc4N3
InChI=1S/C19H21N5O2/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24/h2-8H,9-13H2,1H3,(H,21,26)
Y Key:RMHMFHUVIITRHF-UHFFFAOYSA-N
Y
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 [ ]
^ Stolerman IP (2 August 2010). Encyclopedia of Psychopharmacology . Springer. p. 811. ISBN 978-3-540-68698-9 . Retrieved 26 June 2013 .
^ Czepita D (2005). "[Fundamentals of modern treatment of myopia]". Annales Academiae Medicae Stetinensis . 51 (2): 5–9. PMID 16519089 .
^ Walline, Jeffrey J.; Lindsley, Kristina B.; Vedula, S. Swaroop; Cotter, Susan A.; Mutti, Donald O.; Ng, Sueko M.; Twelker, J. Daniel (13 January 2020). "Interventions to slow progression of myopia in children" . The Cochrane Database of Systematic Reviews . 1 (9): CD004916. doi :10.1002/14651858.CD004916.pub4 . ISSN 1469-493X . PMC 6984636 . PMID 31930781 .
^ Pediani JD, Ward RJ, Godin AG, Marsango S, Milligan G (June 2016). "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs" . The Journal of Biological Chemistry . 291 (25): 13132–46. doi :10.1074/jbc.M115.712562 . PMC 4933229 . PMID 27080256 .
Drugs for peptic ulcer and GERD/GORD (A02B )
H2 antagonists ("-tidine")Prostaglandins (E)/analogues ("-prost-")Proton-pump inhibitors ("-prazole")Potassium-competitive acid blockers ("-prazan") Others Combinations
See also: Helicobacter pylori eradication protocols
# WHO-EM
‡ Withdrawn from market
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† Phase III
§ Never to phase III
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