pirenzepine
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. It has no effects on the brain and spinal cord as it cannot diffuse through the blood–brain barrier. — Wikipedia
Clinical trial activity
4 trials · 3 clinical orgs · 0 marketing orgs
Earliest trial started Aug 1, 2019 (NCT04005287)
Timeline
2010s
- Jan 1, 2019
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Muscarinic acetylcholine receptor M1INHIBITOR
CHRM1 inhibitor
Chemistry & pharmacology
SMILES
CN1CCN(CC(=O)N2c3ccccc3C(=O)Nc3cccnc32)CC1- Mol. weight
- 351.41 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPirenzepine ↗
- ChEMBLCHEMBL9967 ↗
Also known as
- 11-((4-methyl-1-piperazinyl)acetyl)-5,11-dihydro-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one
- 11-((4-methyl-1-piperazinyl)acetyl)-5,11-dihydro-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one
- gastri p
- gastrozepin
- gastrozepin
- pirenzepin
- pirenzepin
- pirenzepin
- pirenzepina
- pirenzepina
- pirenzepine
- pirenzepine
- pirenzepine
- pirenzepine
- pirenzepine
- pirenzepine
- pirenzépine
- pirenzépine
- pirenzepine dihydrochloride
- pirenzepine hcl
- pirenzepine hydrochloride
- pirenzepine hydrochloride hydrate
- pirenzepinum
- pirenzepinum
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05488873 | Phase 2 | Nov 22, 2022 | WinSanTor, Inc |
| NCT05005078 | Phase 2 | Dec 1, 2021 | WinSanTor, Inc |
| NCT04786340 | Phase 2 | Nov 20, 2020 | Eastern Virginia Medical School, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), WinSanTor, Inc |
| NCT04005287 | Phase 2 | Aug 1, 2019 | WinSanTor, Inc |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| WinSanTor, Inc | For profit | 4 | 4 | 1 | 2019 |
| Eastern Virginia Medical School | Academic/Hospital | 1 | 0 | 1 | 2020 |
| National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | Government | 1 | 0 | 1 | 2020 |