Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H21N5O2 |
| Molecular Weight | 351.4023 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCN(CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4)CC1
InChI
InChIKey=RMHMFHUVIITRHF-UHFFFAOYSA-N
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)
Pirenzepine is a M1 muscarinic receptor antagonist, which is prescribed for the treatment of gastric and duodenal ulcer in Europe. The drug preferentially acts on the gastric mucosa to inhibit secretion of both gastric acid and pepsin. Experiment with healthy volunteers demonstrated that pirenzepine passes the blood-brain barrier, but only to a small extent.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P11229 Gene ID: 1128.0 Gene Symbol: CHRM1 Target Organism: Homo sapiens (Human) |
192.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | GASTROZEPIN Approved UseGASTROZEPIN is used for a duodenal ulcer and a benign stomach ulcer. |
|||
| Primary | GASTROZEPIN Approved UseGASTROZEPIN is used for a duodenal ulcer and a benign stomach ulcer. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| A double-blind placebo-controlled case study of the use of donepezil to improve cognition in a schizoaffective disorder patient: functional MRI correlates. | 2001 |
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| Pharmacology, distribution and development of muscarinic acetylcholine receptor subtypes in the optic tectum of Rana pipiens. | 2001 |
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| First experiences in combination therapy using olanzapine with SSRIs (citalopram, paroxetine) in delusional depression. | 2001 |
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| Effect of amantadine on weight gain during olanzapine treatment. | 2001 Apr |
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| Manic symptoms induced by olanzapine. | 2001 Apr |
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| Regulation of phospholipase Cbeta activity by muscarinic acetylcholine and 5-HT(2) receptors in crude and synaptosomal membranes from human cerebral cortex. | 2001 Apr |
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| Comment: olanzapine-induced acute pancreatitis. | 2001 Apr |
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| Olanzapine overdose. | 2001 Apr |
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| Ondansetron for tardive dyskinesia. | 2001 Apr |
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| Neuroleptic malignant syndrome after addition of haloperidol to atypical antipsychotic. | 2001 Apr |
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| Six-month outcomes for patients who switched to olanzapine treatment. | 2001 Apr |
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| Acetylcholine increases the free intracellular calcium concentration in podocytes in intact rat glomeruli via muscarinic M(5) receptors. | 2001 Apr |
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| Olanzapine-associated priapism. | 2001 Apr |
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| Reply to comments on "Olanzapine treatment of children, adolescents, and adults with pervasive developmental disorders: an open-label pilot study". | 2001 Apr |
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| Olanzapine and Huntington's disease. | 2001 Apr |
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| Functional characterization of rat submaxillary gland muscarinic receptors using microphysiometry. | 2001 Apr |
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| Ca(2+) signaling in porcine duodenal glands by muscarinic receptor activation. | 2001 Apr |
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| Acetylcholine increases intracellular Ca2+ in the rat pituitary folliculostellate cells in primary culture. | 2001 Apr |
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| Treatment of psychogenic polydipsia: comparison of risperidone and olanzapine, and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan). | 2001 Feb |
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| [Anti-ulcer drug pirenzepin: new use as an aid for prevention of myopia?]. | 2001 Feb |
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| Long-term olanzapine treatment: weight change and weight-related health factors in schizophrenia. | 2001 Feb |
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| Priapism associated with polypharmacy. | 2001 Feb |
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| Tolerability and effectiveness of atypical antipsychotics in male geriatric inpatients. | 2001 Feb |
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| [Subjective and objective evaluation of treating schizophrenia with classic or atypical drugs]. | 2001 Jan-Feb |
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| [Obsessive-compulsive disorders in adolescents with diagnosed schizophrenia]. | 2001 Jan-Feb |
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| [Viewpoint of schizophrenic patients: a European survey]. | 2001 Jan-Feb |
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| Olanzapine may be an effective adjunctive therapy in the management of acne excoriée: a case report. | 2001 Jan-Feb |
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| Analysis of the QTc interval during olanzapine treatment of patients with schizophrenia and related psychosis. | 2001 Mar |
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| Dementia with Lewy bodies in Down's syndrome. | 2001 Mar |
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| Effects of antimanic mood-stabilizing drugs on fetuses, neonates, and nursing infants. | 2001 Mar |
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| Treatment of posttraumatic stress disorder with olanzapine. | 2001 Mar |
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| Olanzapine-lnduced hyperglycemic nonketonic coma. | 2001 Mar |
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| Serine/threonine protein phosphatases and synaptic inhibition regulate the expression of cholinergic-dependent plateau potentials. | 2001 Mar |
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| Autoantibodies against neonatal heart M1 muscarinic acetylcholine receptor in children with congenital heart block. | 2001 Mar |
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| 5-HT(2A) and D(2) receptor blockade increases cortical DA release via 5-HT(1A) receptor activation: a possible mechanism of atypical antipsychotic-induced cortical dopamine release. | 2001 Mar |
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| Insulin and leptin levels in patients with schizophrenia or related psychoses--a comparison between different antipsychotic agents. | 2001 Mar 1 |
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| Effects of olanzapine and other antipsychotics on cognitive function in chronic schizophrenia: a longitudinal study. | 2001 Mar 1 |
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| The allosteric interaction of otenzepad (AF-DX 116) at muscarinic M2 receptors in guinea pig atria. | 2001 Mar 30 |
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| Quantitative determination of olanzapine in rat brain tissue by high-performance liquid chromatography with electrochemical detection. | 2001 Mar 5 |
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| Separation of olanzapine, carbamazepine and their main metabolites by capillary electrophoresis with pseudo-stationary phases. | 2001 Mar 5 |
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| Haloperidol-stomach lesions attenuation by pentadecapeptide BPC 157, omeprazole, bromocriptine, but not atropine, lansoprazole, pantoprazole, ranitidine, cimetidine and misoprostol in mice. | 2001 Mar 9 |
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| Reversal of pathologic cardiac parameters after transition from clozapine to olanzapine treatment: a case report. | 2001 Mar-Apr |
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| The antinociceptive and sedative effects of carbachol and oxycodone administered into brainstem pontine reticular formation and spinal subarachnoid space in rats. | 2001 May |
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| Nitric oxide modulates cardiac performance in the heart of Anguilla anguilla. | 2001 May |
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| Expression of multiple subtypes of muscarinic receptors and cellular distribution in the human heart. | 2001 May |
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| Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity. | 2001 May |
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| Molecular and pharmacological characterization of muscarinic receptor subtypes in a rat parotid gland cell line: comparison with native parotid gland. | 2001 May |
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| Long-term effects of olanzapine, risperidone, and quetiapine on dopamine receptor types in regions of rat brain: implications for antipsychotic drug treatment. | 2001 May |
|
| Agonist activation of cytosolic Ca2+ in subfornical organ cells projecting to the supraoptic nucleus. | 2001 May |
|
| Antibodies against human putamen in adolescents with anorexia nervosa. | 2001 May |
Patents
Sample Use Guides
Gastric and duodenal ulcers: 1 tablet (GASTROZEPIN 50 mg) 2 times daily (morning and evening). Severe and complicated gastric and duodenal ulcers: 1 tablet (GASTROZEPINE 50 mg) 3 times daily.
Route of Administration:
Oral
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A02BX03
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NCI_THESAURUS |
C29704
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WHO-VATC |
QA02BX03
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D010890
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28797-61-7
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100000081663
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2200
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DB00670
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4848
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m8874
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PIRENZEPINE
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DTXSID7023487
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328
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3G0285N20N
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CHEMBL9967
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C76002
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8352
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8247
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3476
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SUB09904MIG
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249-228-4
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)
