Pirenzepine
Chemical compound
- A02BX03 (WHO)
- 11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
- 28797-61-7
Y
- 4848
- 328
- DB00670 Y
- 4682 Y
- 3G0285N20N
- D08389 Y
- CHEBI:8247 Y
- ChEMBL9967 Y
- DTXSID7023487
- Interactive image
- O=C3c1ccccc1N(C(=O)CN2CCN(C)CC2)c4ncccc4N3
InChI
- 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-NY
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
- ^ 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 JJ, Lindsley KB, Vedula SS, Cotter SA, Mutti DO, Ng SM, Twelker JD (January 2020). "Interventions to slow progression of myopia in children". The Cochrane Database of Systematic Reviews. 1 (1): CD004916. doi:10.1002/14651858.CD004916.pub4. 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): 13132–13146. doi:10.1074/jbc.M115.712562. PMC 4933229. PMID 27080256.
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analogues ("-prost-")
("-prazole")
acid blockers ("-prazan")
- Linaprazan
- Revaprazan
- Soraprazan
- Vonoprazan
- See also: Helicobacter pylori eradication protocols
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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