Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H21N5O2.2ClH.H2O |
| Molecular Weight | 442.3401 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCN(CC1)CC(=O)N2c3ccccc3C(=Nc4cccnc42)O.Cl.Cl.O
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 | ClH |
| Molecular Weight | 36.4609 |
| 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 | C19H21N5O2 |
| Molecular Weight | 351.4031 |
| 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 |
|---|---|---|
| Pharmacology, distribution and development of muscarinic acetylcholine receptor subtypes in the optic tectum of Rana pipiens. | 2001 |
|
| First experiences in combination therapy using olanzapine with SSRIs (citalopram, paroxetine) in delusional depression. | 2001 |
|
| Weight change and atypical antipsychotic treatment in patients with schizophrenia. | 2001 |
|
| An efficacy analysis of olanzapine treatment data in schizophrenia patients with catatonic signs and symptoms. | 2001 |
|
| Effective resolution with olanzapine of acute presentation of behavioral agitation and positive psychotic symptoms in schizophrenia. | 2001 |
|
| Manic symptoms induced by olanzapine. | 2001 Apr |
|
| Neuroleptic malignant syndrome after addition of haloperidol to atypical antipsychotic. | 2001 Apr |
|
| Six-month outcomes for patients who switched to olanzapine treatment. | 2001 Apr |
|
| Acetylcholine increases the free intracellular calcium concentration in podocytes in intact rat glomeruli via muscarinic M(5) receptors. | 2001 Apr |
|
| Olanzapine-associated priapism. | 2001 Apr |
|
| Olanzapine and Huntington's disease. | 2001 Apr |
|
| Acetylcholine increases intracellular Ca2+ in the rat pituitary folliculostellate cells in primary culture. | 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 |
|
| [Anti-ulcer drug pirenzepin: new use as an aid for prevention of myopia?]. | 2001 Feb |
|
| Long-term olanzapine treatment: weight change and weight-related health factors in schizophrenia. | 2001 Feb |
|
| Priapism associated with polypharmacy. | 2001 Feb |
|
| Tolerability and effectiveness of atypical antipsychotics in male geriatric inpatients. | 2001 Feb |
|
| Fully automated on-line determination of olanzapine in serum for routine therapeutic drug monitoring. | 2001 Feb |
|
| Effects of newer atypical antipsychotics on autonomic neurocardiac function: a comparison between amisulpride, olanzapine, sertindole, and clozapine. | 2001 Feb |
|
| The economic consequences of a drug-drug interaction. | 2001 Feb |
|
| Repeated episodes of hypothermia in a subject treated with haloperidol, levomepromazine, olanzapine, and thioridazine. | 2001 Feb |
|
| Atypical antipsychotics and cardiovascular risk in schizophrenic patients. | 2001 Feb |
|
| Pharmacological characterization of muscarinic receptors in dog isolated ciliary and urinary bladder smooth muscle. | 2001 Feb |
|
| Traditional and new antipsychotic drugs differentially alter neurotransmission markers in basal ganglia-thalamocortical neural pathways. | 2001 Feb |
|
| Characterisation of the prejunctional inhibitory muscarinic receptor on cholinergic nerves in the rat urinary bladder. | 2001 Feb 16 |
|
| The effects of olanzapine in reducing the emergence of psychosis among nursing home patients with Alzheimer's disease. | 2001 Jan |
|
| Bodyweight gain with atypical antipsychotics. A comparative review. | 2001 Jan |
|
| Allelic variation in the 5-HT2C receptor (HT2RC) and the increase in slow wave sleep produced by olanzapine. | 2001 Jan 1 |
|
| 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 |
|
| [Subjective and objective evaluation of treating schizophrenia with classic or atypical drugs]. | 2001 Jan-Feb |
|
| [Obsessive-compulsive disorders in adolescents with diagnosed schizophrenia]. | 2001 Jan-Feb |
|
| Olanzapine may be an effective adjunctive therapy in the management of acne excoriée: a case report. | 2001 Jan-Feb |
|
| Analysis of the QTc interval during olanzapine treatment of patients with schizophrenia and related psychosis. | 2001 Mar |
|
| Dementia with Lewy bodies in Down's syndrome. | 2001 Mar |
|
| Effects of antimanic mood-stabilizing drugs on fetuses, neonates, and nursing infants. | 2001 Mar |
|
| Treatment of posttraumatic stress disorder with olanzapine. | 2001 Mar |
|
| Olanzapine-lnduced hyperglycemic nonketonic coma. | 2001 Mar |
|
| Serine/threonine protein phosphatases and synaptic inhibition regulate the expression of cholinergic-dependent plateau potentials. | 2001 Mar |
|
| Autoantibodies against neonatal heart M1 muscarinic acetylcholine receptor in children with congenital heart block. | 2001 Mar |
|
| Atypical antipsychotics and hyperglycaemia. | 2001 Mar |
|
| Low blood glucose and olanzapine. | 2001 Mar |
|
| Does fast dissociation from the dopamine d(2) receptor explain the action of atypical antipsychotics?: A new hypothesis. | 2001 Mar |
|
| Insulin and leptin levels in patients with schizophrenia or related psychoses--a comparison between different antipsychotic agents. | 2001 Mar 1 |
|
| Quantitative determination of olanzapine in rat brain tissue by high-performance liquid chromatography with electrochemical detection. | 2001 Mar 5 |
|
| Separation of olanzapine, carbamazepine and their main metabolites by capillary electrophoresis with pseudo-stationary phases. | 2001 Mar 5 |
|
| Haloperidol-stomach lesions attenuation by pentadecapeptide BPC 157, omeprazole, bromocriptine, but not atropine, lansoprazole, pantoprazole, ranitidine, cimetidine and misoprostol in mice. | 2001 Mar 9 |
|
| Reversal of pathologic cardiac parameters after transition from clozapine to olanzapine treatment: a case report. | 2001 Mar-Apr |
|
| 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 |
|
| Long-term effects of olanzapine, risperidone, and quetiapine on dopamine receptor types in regions of rat brain: implications for antipsychotic drug treatment. | 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
Fri Jun 25 20:42:20 UTC 2021
by
admin
on
Fri Jun 25 20:42:20 UTC 2021
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| Record UNII |
TR66JMA2FS
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| Record Status |
Validated (UNII)
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| Record Version |
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SUB12219MIG
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TR66JMA2FS
Created by
admin on Fri Jun 25 20:42:20 UTC 2021 , Edited by admin on Fri Jun 25 20:42:20 UTC 2021
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