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Chemical compound
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]
^ 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 .
mAChRs Tooltip Muscarinic acetylcholine receptors
Agonists Antagonists
3-Quinuclidinyl benzilate
4-DAMP
Aclidinium bromide (+formoterol )
Abediterol
AF-DX 250
AF-DX 384
Ambutonium bromide
Anisodamine
Anisodine
Antihistamines (first-generation) (e.g., brompheniramine , buclizine , captodiame , chlorphenamine (chlorpheniramine) , cinnarizine , clemastine , cyproheptadine , dimenhydrinate , dimetindene , diphenhydramine , doxylamine , meclizine , mequitazine , perlapine , phenindamine , pheniramine , phenyltoloxamine , promethazine , propiomazine , triprolidine )
AQ-RA 741
Atropine
Atropine methonitrate
Atypical antipsychotics (e.g., clozapine , fluperlapine , olanzapine (+fluoxetine ), rilapine , quetiapine , tenilapine , zotepine )
Benactyzine
Benzatropine (benztropine)
Benzilone
Benzilylcholine mustard
Benzydamine
Bevonium
BIBN 99
Biperiden
Bornaprine
Camylofin
CAR-226,086
CAR-301,060
CAR-302,196
CAR-302,282
CAR-302,368
CAR-302,537
CAR-302,668
Caramiphen
Cimetropium bromide
Clidinium bromide
Cloperastine
CS-27349
Cyclobenzaprine
Cyclopentolate
Darifenacin
DAU-5884
Desfesoterodine
Dexetimide
DIBD
Dicycloverine (dicyclomine)
Dihexyverine
Difemerine
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Ditran
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EA-3167
EA-3443
EA-3580
EA-3834
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Hexahydrodifenidol
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Hexbutinol
Hexocyclium
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HL-031,120
Homatropine
Imidafenacin
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Isopropamide
J-104,129
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Mamba toxin 3
Mamba toxin 7
Mazaticol
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Methylscopolamine
Metixene
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PBID
PD-102,807
PD-0298029
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Pethidine
pFHHSiD
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Phenyltoloxamine
Pipenzolate bromide
Piperidolate
Pirenzepine
Piroheptine
Pizotifen
Poldine
Pridinol
Prifinium bromide
Procyclidine
Profenamine (ethopropazine)
Propantheline bromide
Propiverine
Quinidine
3-Quinuclidinyl thiochromane-4-carboxylate
Revefenacin
Rociverine
RU-47,213
SCH-57,790
SCH-72,788
SCH-217,443
Scopolamine (hyoscine)
Scopolamine butylbromide (hyoscine butylbromide)
Silahexacyclium
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Solifenacin
SSRIs Tooltip Selective serotonin reuptake inhibitors (e.g., femoxetine , paroxetine )
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Tetracyclic antidepressants (e.g., amoxapine , maprotiline , mianserin , mirtazapine )
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Timepidium bromide
Tiotropium bromide
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Tolterodine
Tricyclic antidepressants (e.g., amitriptyline (+perphenazine ), amitriptylinoxide , butriptyline , cidoxepin , clomipramine , desipramine , desmethyldesipramine , dibenzepin , dosulepin (dothiepin) , doxepin , imipramine , lofepramine , nitroxazepine , northiaden (desmethyldosulepin) , nortriptyline , protriptyline , quinupramine , trimipramine )
Tridihexethyl
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Tropicamide
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Typical antipsychotics (e.g., chlorpromazine , chlorprothixene , cyamemazine (cyamepromazine) , loxapine , mesoridazine , thioridazine )
Umeclidinium bromide (+vilanterol )
WIN-2299
Xanomeline
Zamifenacin
Precursors (and prodrugs )