Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H21N5O2.2ClH.H2O |
| Molecular Weight | 442.34 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.Cl.Cl.CN1CCN(CC(=O)N2C3=C(C=CC=C3)C(=O)NC4=C2N=CC=C4)CC1
InChI
InChIKey=ZOAVUHCVXFVQOA-UHFFFAOYSA-N
InChI=1S/C19H21N5O2.2ClH.H2O/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);2*1H;1H2
| Molecular Formula | C19H21N5O2 |
| Molecular Weight | 351.4023 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|
| First experiences in combination therapy using olanzapine with SSRIs (citalopram, paroxetine) in delusional depression. | 2001 |
|
| Superior efficacy of olanzapine over haloperidol: analysis of patients with schizophrenia from a multicenter international trial. | 2001 |
|
| Cardiac safety parameters of olanzapine: comparison with other atypical and typical antipsychotics. | 2001 |
|
| Introduction: a new era in the pharmacotherapy of psychotic disorders. | 2001 |
|
| Evidence for the effectiveness of olanzapine among patients nonresponsive and/or intolerant to risperidone. | 2001 |
|
| An efficacy analysis of olanzapine treatment data in schizophrenia patients with catatonic signs and symptoms. | 2001 |
|
| Effect of amantadine on weight gain during olanzapine treatment. | 2001 Apr |
|
| Reply to comments on "Olanzapine treatment of children, adolescents, and adults with pervasive developmental disorders: an open-label pilot study". | 2001 Apr |
|
| Olanzapine and Huntington's disease. | 2001 Apr |
|
| Functional characterization of rat submaxillary gland muscarinic receptors using microphysiometry. | 2001 Apr |
|
| Treatment of psychogenic polydipsia: comparison of risperidone and olanzapine, and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan). | 2001 Feb |
|
| Olanzapine and hypertriglyceridemia. | 2001 Feb |
|
| Effects of newer atypical antipsychotics on autonomic neurocardiac function: a comparison between amisulpride, olanzapine, sertindole, and clozapine. | 2001 Feb |
|
| Repeated episodes of hypothermia in a subject treated with haloperidol, levomepromazine, olanzapine, and thioridazine. | 2001 Feb |
|
| Muscarinic receptor subtypes and calcium signaling in Fischer rat thyroid cells. | 2001 Feb 1 |
|
| Bodyweight gain with atypical antipsychotics. A comparative review. | 2001 Jan |
|
| Misdiagnosis of schizophrenia for a patient with epilepsy. | 2001 Jan |
|
| A novel augmentation strategy for treating resistant major depression. | 2001 Jan |
|
| Lowered seizure threshold on olanzapine. | 2001 Jan |
|
| Secretion and gene expression of secretory leukocyte protease inhibitor by human airway submucosal glands. | 2001 Jan |
|
| Allelic variation in the 5-HT2C receptor (HT2RC) and the increase in slow wave sleep produced by olanzapine. | 2001 Jan 1 |
|
| Consistency of atypical antipsychotic superiority to placebo in recent clinical trials. | 2001 Jan 1 |
|
| Interleukin-2 and interleukin-4 increase the survival of retinal ganglion cells in culture. | 2001 Jan 22 |
|
| A sensitive high-performance liquid chromatographic method using electrochemical detection for the analysis of olanzapine and desmethylolanzapine in plasma of schizophrenic patients using a new solid-phase extraction procedure. | 2001 Jan 5 |
|
| [Viewpoint of schizophrenic patients: a European survey]. | 2001 Jan-Feb |
|
| A predicted cortical serotonergic/cholinergic/GABAergic interface as a site of pathology in schizophrenia. | 2001 Jan-Feb |
|
| Dementia with Lewy bodies in Down's syndrome. | 2001 Mar |
|
| Olanzapine-lnduced hyperglycemic nonketonic coma. | 2001 Mar |
|
| 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 |
|
| Insulin and leptin levels in patients with schizophrenia or related psychoses--a comparison between different antipsychotic agents. | 2001 Mar 1 |
|
| The allosteric interaction of otenzepad (AF-DX 116) at muscarinic M2 receptors in guinea pig atria. | 2001 Mar 30 |
|
| The antinociceptive and sedative effects of carbachol and oxycodone administered into brainstem pontine reticular formation and spinal subarachnoid space in rats. | 2001 May |
|
| Nitric oxide modulates cardiac performance in the heart of Anguilla anguilla. | 2001 May |
|
| 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 |
|
| 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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:32:39 UTC 2023
by
admin
on
Sat Dec 16 07:32:39 UTC 2023
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| Record UNII |
TR66JMA2FS
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| Record Status |
Validated (UNII)
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100000079628
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SUB12219MIG
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TR66JMA2FS
Created by
admin on Sat Dec 16 07:32:39 UTC 2023 , Edited by admin on Sat Dec 16 07:32:39 UTC 2023
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ANHYDROUS->SOLVATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |