pirenzepine

Summary

Summary: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.

Top Publications

  1. Carlson C, Cavazzoni P, Berg P, Wei H, Beasley C, Kane J. An integrated analysis of acute treatment-emergent extrapyramidal syndrome in patients with schizophrenia during olanzapine clinical trials: comparisons with placebo, haloperidol, risperidone, or clozapine. J Clin Psychiatry. 2003;64:898-906 pubmed
    ..040) and significantly shorter among clozapine-treated patients (p =.021). This analysis of available data from olanzapine clinical trials lends additional support to olanzapine's favorable EPS profile. ..
  2. Le Q, Cheng N, Wu W, Chu R. Effect of pirenzepine ophthalmic solution on form-deprivation myopia in the guinea pigs. Chin Med J (Engl). 2005;118:561-6 pubmed
    ..study was to determine the efficacy, through topical administration, of the M1-selective muscarinic antagonist pirenzepine in preventing experimentally induced form-deprivation myopia in guinea pigs...
  3. Tan D, Lam D, Chua W, Shu Ping D, Crockett R. One-year multicenter, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia. Ophthalmology. 2005;112:84-91 pubmed
    To evaluate the safety and efficacy of the relatively selective M(1)-antagonist, pirenzepine ophthalmic gel (gel), in slowing the progression of myopia in school-aged children...
  4. Gwiazda J. Treatment options for myopia. Optom Vis Sci. 2009;86:624-8 pubmed publisher
    ..various types of spectacle lenses and contact lenses, as well as pharmaceutical agents such as atropine and pirenzepine. The bulk of evidence from well-conducted studies shows that overall, most therapies for myopia have small ..
  5. Theisen F, Haberhausen M, Schulz E, Fleischhaker C, Clement H, Heinzel Gutenbrunner M, et al. Serum levels of olanzapine and its N-desmethyl and 2-hydroxymethyl metabolites in child and adolescent psychiatric disorders: effects of dose, diagnosis, age, sex, smoking, and comedication. Ther Drug Monit. 2006;28:750-9 pubmed
    ..The data are compared with the literature, and the relevance of therapeutic antipsychotic drug monitoring in previously sparsely investigated subgroups, such as children and adolescents or patients with AN, is emphasized. ..
  6. Sato Y, Inoue S, Katagiri F, Itoh H, Takeyama M. Effects of pirenzepine on Dai-kenchu-to-induced elevation of the plasma neuropeptide levels in humans. Biol Pharm Bull. 2006;29:166-71 pubmed
    ..We examined the effects of the selective M(1) muscarinic receptor antagonist pirenzepine on the elevation of Dai-kenchu-to-induced plasma neuropeptide (gastrin, motilin, somatostatin, VIP, CGRP, ..
  7. Siatkowski R, Cotter S, Miller J, Scher C, Crockett R, Novack G. Safety and efficacy of 2% pirenzepine ophthalmic gel in children with myopia: a 1-year, multicenter, double-masked, placebo-controlled parallel study. Arch Ophthalmol. 2004;122:1667-74 pubmed
    To evaluate the safety and efficacy of the relatively selective M(1) antagonist pirenzepine hydrochloride in slowing the progression of myopia in school-aged children...
  8. Chin C, Zhang Z, Karnes H. A study of matrix effects on an LC/MS/MS assay for olanzapine and desmethyl olanzapine. J Pharm Biomed Anal. 2004;35:1149-67 pubmed
    ..Differential behavior between the analytes and labeled internal standards contributed to variability. The most significant source of variability however, was ion suppression due to co-eluting matrix components. ..
  9. Moreira K, Hipólide D, Nobrega J, Bueno O, Tufik S, Oliveira M. Deficits in avoidance responding after paradoxical sleep deprivation are not associated with altered [3H]pirenzepine binding to M1 muscarinic receptors in rat brain. Brain Res. 2003;977:31-7 pubmed
    ..are observed in non-deprived rats after treatment with M1-selective antagonist compounds such as dicyclomine or pirenzepine cause similar impairments, and gave rise to the hypothesis that sleep deprivation might induce significant ..

More Information

Publications99

  1. Josefsson M, Roman M, Skogh E, Dahl M. Liquid chromatography/tandem mass spectrometry method for determination of olanzapine and N-desmethylolanzapine in human serum and cerebrospinal fluid. J Pharm Biomed Anal. 2010;53:576-82 pubmed publisher
    ..The method was successfully used for the analysis of samples from patients treated with olanzapine in the dose range of 2.5-25mg/day. ..
  2. Siatkowski R, Cotter S, Crockett R, Miller J, Novack G, Zadnik K. Two-year multicenter, randomized, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia. J AAPOS. 2008;12:332-9 pubmed publisher
    To evaluate if the safety and efficacy of the relatively selective M1-antagonist, pirenzepine, in slowing the progression of myopia in children is sustained over a 2-year period...
  3. Carr D, Surmeier D. M1 muscarinic receptor modulation of Kir2 channels enhances temporal summation of excitatory synaptic potentials in prefrontal cortex pyramidal neurons. J Neurophysiol. 2007;97:3432-8 pubmed
    ..As a consequence of this dual modulation, the responses to a single, isolated afferent volley was reduced, but the response to a high-frequency afferent burst was potentiated...
  4. Tahtaoui C, Parrot I, Klotz P, Guillier F, Galzi J, Hibert M, et al. Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor. J Med Chem. 2004;47:4300-15 pubmed
    ..between enhanced green fluorescent protein (EGFP)-fused human muscarinic M1 receptors and Bodipy-labeled pirenzepine, we synthesized seven fluorescent derivatives of this antagonist in order to further characterize ligand-..
  5. Ouyang C, Chu R, Hu W. [Effects of pirenzepine on lens-induced myopia in the guinea-pig]. Zhonghua Yan Ke Za Zhi. 2003;39:348-51 pubmed
    To determine the efficacy of the M(1)-selective muscarinic antagonist, pirenzepine, in preventing lens-induced myopia in the guinea-pig and to study the mechanism and the possibility of treatment of myopia with pirenzepine...
  6. Ilien B, Glasser N, Clamme J, Didier P, Piemont E, Chinnappan R, et al. Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process. J Biol Chem. 2009;284:19533-43 pubmed publisher
    ..We report here, using a combination of fluorescence approaches, on the molecular mechanisms for Bodipy-pirenzepine binding to enhanced green fluorescent protein (EGFP)-fused muscarinic M1 receptors in living cells...
  7. Truong H, Cottriall C, Gentle A, McBrien N. Pirenzepine affects scleral metabolic changes in myopia through a non-toxic mechanism. Exp Eye Res. 2002;74:103-11 pubmed
    ..has been shown that various pharmacological agents, including the muscarinic receptor antagonists, atropine and pirenzepine, are effective at preventing the development of myopia...
  8. Skogh E, Reis M, Dahl M, Lundmark J, Bengtsson F. Therapeutic drug monitoring data on olanzapine and its N-demethyl metabolite in the naturalistic clinical setting. Ther Drug Monit. 2002;24:518-26 pubmed
    ..The present TDM-based follow-up suggests that the influence of gender, smoking habits, and certain drug interactions may need to be considered for optimal dosage of OLA. TDM may be used for this purpose more readily in the future. ..
  9. Saw S, Gazzard G, Au Eong K, Tan D. Myopia: attempts to arrest progression. Br J Ophthalmol. 2002;86:1306-11 pubmed
  10. Piggott M, Owens J, O BRIEN J, Paling S, Wyper D, Fenwick J, et al. Comparative distribution of binding of the muscarinic receptor ligands pirenzepine, AF-DX 384, (R,R)-I-QNB and (R,S)-I-QNB to human brain. J Chem Neuroanat. 2002;24:211-23 pubmed
    ..We have compared the in vitro binding of the muscarinic ligands [3H]pirenzepine and [3H]AF-DX 384, which have selectivity for the M1 and M2/M4 receptor subtypes, respectively, to the binding ..
  11. Cottriall C, Truong H, McBrien N. Inhibition of myopia development in chicks using himbacine: a role for M(4) receptors?. Neuroreport. 2001;12:2453-6 pubmed
    The success of the M(1)-selective muscarinic antagonist pirenzepine in preventing myopia development in animal models implicates a role for the M(1) receptor...
  12. Fontaine C, Hynan L, Koch K, Martin Cook K, Svetlik D, Weiner M. A double-blind comparison of olanzapine versus risperidone in the acute treatment of dementia-related behavioral disturbances in extended care facilities. J Clin Psychiatry. 2003;64:726-30 pubmed
    ..Low-dose, once-a-day olanzapine and risperidone appear to be equally safe and equally effective in the treatment of dementia-related behavioral disturbances in residents of extended care facilities. ..
  13. Hartfield A, Moore N, Clifton P. Effects of clozapine, olanzapine and haloperidol on the microstructure of ingestive behaviour in the rat. Psychopharmacology (Berl). 2003;167:115-22 pubmed
    ..Conversely, haloperidol leaves satiety unaffected but reduces the palatability of the fat emulsion resulting in reduced intake. ..
  14. Landi F, Cesari M, Zuccalà C, Barillaro C, Cocchi A. Olanzapine and hypoglycemic coma in a frail elderly woman. A case report. Pharmacopsychiatry. 2003;36:165-6 pubmed
  15. López Mato A, Rovner J, Illa G, Vieitez A, Boullosa O. [Randomized, open label study on the use of ranitidine at different doses for the management of weight gain associated with olanzapine administration]. Vertex. 2003;14:85-96 pubmed
    ..The risk/benefit ratio is a paradigm in the practice of medicine. In the case of Olanzapine, the scale clearly tips in favor of the latter, making it the drug of choice in the treatment of schizophrenia and other psychotic disorders. ..
  16. Orii R, Sugawara Y, Sawamura S, Yamada Y. M?muscarinic receptors mediate acetylcholine-induced pulmonary vasodilation in pulmonary hypertension. Biosci Trends. 2010;4:260-6 pubmed
    ..The effects of cumulative concentrations of three specific muscarinic receptor subtype antagonists [pirenzepine (M?), methoctramine (M?), and 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, M?] on ACh-induced ..
  17. Fumagalli F, Molteni R, Roceri M, Bedogni F, Santero R, Fossati C, et al. Effect of antipsychotic drugs on brain-derived neurotrophic factor expression under reduced N-methyl-D-aspartate receptor activity. J Neurosci Res. 2003;72:622-8 pubmed
  18. Bilgen I, Oner G, Edremitlioglu M, Alkan Z, Cirrik S. Involvement of cholinoceptors in cadmium-induced endothelial dysfunction. J Basic Clin Physiol Pharmacol. 2003;14:55-76 pubmed
    ..Cadmium decreased both the maximal response to ACh (10(-5) M) and its pirenzepine (Prz) sensitive component...
  19. Brandish P, Hill L, Zheng W, Scolnick E. Scintillation proximity assay of inositol phosphates in cell extracts: high-throughput measurement of G-protein-coupled receptor activation. Anal Biochem. 2003;313:311-8 pubmed
    ..Further, we demonstrate the use and functional validity of this assay in a semiautomated, 384-well format, by characterizing the muscarinic receptor antagonists pirenzepine and atropine.
  20. Martin Escudero J, Duenas Laita A, Perez Castrillon J, Herreros Fernández V. Olanzapine toxicity in unconjugated hyperbilirubinaemia (Gilbert's syndrome). Br J Psychiatry. 2003;182:267 pubmed
  21. Seillier A, Coutureau E, Thiriet N, Herbeaux K, Zwiller J, Di Scala G, et al. Bilateral lesions of the entorhinal cortex differentially modify haloperidol- and olanzapine-induced c-fos mRNA expression in the rat forebrain. Neuropharmacology. 2003;45:190-200 pubmed
    ..Our results further emphasize the importance of the exploration of the mechanisms of action of antipsychotic drugs in the context of an associated cortical pathology. ..
  22. Newell K, Zavitsanou K, Huang X. Opposing short- and long-term effects on muscarinic M1/4 receptor binding following chronic phencyclidine treatment. J Neurosci Res. 2007;85:1358-63 pubmed
    ..3)H]pirenzepine was used to target M1/4 receptors...
  23. Ebenbichler C, Laimer M, Eder U, Mangweth B, Weiss E, Hofer A, et al. Olanzapine induces insulin resistance: results from a prospective study. J Clin Psychiatry. 2003;64:1436-9 pubmed
    ..However, beta cell function remains unaltered in olanzapine-treated patients. We conclude that treatment with some second-generation antipsychotic drugs may lead to insulin resistance. ..
  24. Kogoj A, Velikonja I. Olanzapine induced neuroleptic malignant syndrome--a case review. Hum Psychopharmacol. 2003;18:301-9 pubmed
    ..It was found that prior NMS is an important risk factor in NMS. ..
  25. Kinon B, Hill A, Liu H, Kollack Walker S. Olanzapine orally disintegrating tablets in the treatment of acutely ill non-compliant patients with schizophrenia. Int J Neuropsychopharmacol. 2003;6:97-102 pubmed
    ..05). Olanzapine orally disintegrating tablets were well-tolerated. Olanzapine orally disintegrating tablets may benefit acutely ill, non-compliant schizophrenic patients by facilitating acceptance of active antipsychotic drug therapy. ..
  26. Stevens L, Chapple C, Chess Williams R. Human idiopathic and neurogenic overactive bladders and the role of M2 muscarinic receptors in contraction. Eur Urol. 2007;52:531-8 pubmed
    ..The affinities of a range of subtype selective antagonists (DAMP, darifenacin, methoctramine R0-320-6206, and pirenzepine) were obtained in tissue bath experiments by using carbachol as the agonist...
  27. Cui Y, Zhu L, Wang H, Advenier C, Chen H, Devillier P. Muscarinic receptors involved in airway vascular leakage induced by experimental gastro-oesophageal reflux. Life Sci. 2008;82:949-55 pubmed publisher
    ..pretreatment with atropine, a non-specific muscarinic receptor antagonist, and also by pretreatment with either pirenzepine, a muscarinic M(1) receptor antagonist, or 4-DAMP, a muscarinic M(3) receptor antagonist...
  28. Heresco Levy U, Ermilov M, Lichtenberg P, Bar G, Javitt D. High-dose glycine added to olanzapine and risperidone for the treatment of schizophrenia. Biol Psychiatry. 2004;55:165-71 pubmed
  29. Torkkeli P, Widmer A, Meisner S. Expression of muscarinic acetylcholine receptors and choline acetyltransferase enzyme in cultured antennal sensory neurons and non-neural cells of the developing moth Manduca sexta. J Neurobiol. 2005;62:316-29 pubmed
    ..These findings suggest muscarinic cholinergic interactions between the neural and non-neural cells during the development of Manduca antenna. ..
  30. Weisman R. Quetiapine in the successful treatment of schizophrenia with comorbid alcohol and drug dependence: a case report. Int J Psychiatry Med. 2003;33:85-9 pubmed
    ..The possible utility of atypical antipsychotics in the treatment of patients with schizophrenia and comorbid substance abuse needs to be confirmed in clinical trials. ..
  31. Grailhe R, Cardona A, Even N, Seif I, Changeux J, Cloëz Tayarani I. Regional changes in the cholinergic system in mice lacking monoamine oxidase A. Brain Res Bull. 2009;78:283-9 pubmed publisher
    ..Binding of [(125)I]-epibatidine ([(125)I]-Epi), [(125)I]-alpha-bungarotoxin ([(125)I]-BGT), [(3)H]-pirenzepine ([(3)H]-PZR), and [(3)H]-AFDX-384 ([(3)H]-AFX), which respectively label high- and low-affinity nicotinic ..
  32. Zefirov T, Ziyatdinova N, Saifutdinova L, Zefirov A. Cardiac activity and blood pressure in rats during selective blockade of various subtypes of muscarinic cholinoceptors. Bull Exp Biol Med. 2006;141:662-5 pubmed
    ..Our results indicate that muscarinic cholinoceptors play a role in the immediate inhibition of cardiac activity upon vagus nerve stimulation...
  33. Motsinger C, Perron G, Lacy T. Use of atypical antipsychotic drugs in patients with dementia. Am Fam Physician. 2003;67:2335-40 pubmed
    ..Informed use of atypical antipsychotic drugs allows family physicians to greatly improve quality of life in elderly patients with dementia and behavior disturbances. ..
  34. Romański K. Does the cholinergic system modulate gastrointestinal slow waves during less active phases of migrating myoelectric complex in healthy rams?. Folia Med Cracov. 2003;44:79-91 pubmed
    ..of the migrating myoelectric complex (MMC) (carbachol) and during phase 1-2a MMC (hexamethonium, atropine and pirenzepine). Antral slow wave amplitude was unaltered by cholinergic drugs with some exceptions...
  35. Shapovalova K, Kamkina Y, Mysovskii D. The effects of microinjection of the selective blocker of muscarinic M1 receptors pirenzepine into the neostriatum on the motor behavior of rats. Neurosci Behav Physiol. 2005;35:589-94 pubmed
    ..in 18 rats to study the effects of bilateral microinjections of the selective muscarinic M1 receptor blocker pirenzepine into the neostriatum on the acquisition of the CAAR and behavior in an open field test...
  36. Yano K, Koda K, Ago Y, Kobayashi H, Kawasaki T, Takuma K, et al. Galantamine improves apomorphine-induced deficits in prepulse inhibition via muscarinic ACh receptors in mice. Br J Pharmacol. 2009;156:173-80 pubmed publisher
    ..Galantamine improves apomorphine-induced PPI deficits by stimulating mAChRs through increasing brain ACh levels via a dopamine D(1) receptor-dependent mechanism and AChE inhibition. ..
  37. Inan S, Dun N, Cowan A. Investigation of gastrin-releasing peptide as a mediator for 5'-guanidinonaltrindole-induced compulsive scratching in mice. Peptides. 2011;32:286-92 pubmed publisher
    ..We conclude that (a) the GRP receptor system does not mediate GNTI-induced scratching and (b) the kappa opioid system is involved, at least in part, in the scratch suppressing activity of nalfurafine. ..
  38. Hamrouni A, Gudka N, Broadley K. Investigation of the mechanism for the relaxation of rat duodenum mediated via M1 muscarinic receptors. Auton Autacoid Pharmacol. 2006;26:275-84 pubmed
    ..relaxation of the duodenum were of the M1 subtype, the susceptibility to the selective competitive antagonist, pirenzepine and the selective muscarinic toxin from green mamba, MT7, was examined...
  39. du Bois T, Newell K, Han M, Deng C, Huang X. Perinatal PCP treatment alters the developmental expression of prefrontal and hippocampal muscarinic receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2009;33:37-40 pubmed publisher
    ..c.) or saline on postnatal days (PN)7, 9 and 11. [3H]Pirenzepine binding to M1/4 receptors was examined at four time-points (PN12, 18, 32 and 96) following treatment cessation...
  40. Martins S, Moulas G, Trabuco J, Monteiro G, Chu V, Conde J, et al. Monitoring intracellular calcium in response to GPCR activation using thin-film silicon photodiodes with integrated fluorescence filters. Biosens Bioelectron. 2014;52:232-8 pubmed publisher
    ..Using the new device it was possible to characterize the potency of carbachol (EC50=10.5 µM) and pirenzepine (IC50=4.2 ?M), with the same accuracy as standard microscopy optical systems...
  41. Yabuki Y, Jing X, Fukunaga K. The T-type calcium channel enhancer SAK3 inhibits neuronal death following transient brain ischemia via nicotinic acetylcholine receptor stimulation. Neurochem Int. 2017;108:272-281 pubmed publisher
    ..0 mg/kg, i.p.), but not the M1 muscarinic ACh receptor (mAChR) antagonist pirenzepine (PZ: 10 mg/kg, i.p.), blocked enhanced Akt activity elicited by SAK3 (0.5 mg/kg, p.o.)...
  42. Keck P. Long-term therapy of bipolar illness. J Fam Pract. 2003;Suppl:S18-21 pubmed
  43. Issa B, Davies N, Hood K, Premawardhana L, Peters J, Scanlon M. Effect of 2-week treatment with pirenzepine on fasting and postprandial glucose concentrations in individuals with type 2 diabetes. Diabetes Care. 2003;26:1636-7 pubmed
  44. Montgomery A, Grottick A, Herberg L. Alpha2-adrenoceptor antagonism is neither sufficient nor necessary for the distinctive action of atypical neuroleptics on intracranial self-stimulation in the rat. Behav Pharmacol. 2003;14:307-14 pubmed
    ..Various other explanations remain possible, but the accelerated time course of the atypical agents appears to support more recent explanations, based on their rapid dissociation from the D2 receptor. ..
  45. Doi Y, Murasaki O, Kaibara M, Uezono Y, Hayashi H, Yano K, et al. Characterization of functional effects of Z-338, a novel gastroprokinetic agent, on the muscarinic M1, M2, and M3 receptors expressed in Xenopus oocytes. Eur J Pharmacol. 2004;505:31-5 pubmed
    ..These results indicate that Z-338 is a potent antagonist not for muscarinic M3 receptor but for both muscarinic M1 and M2 receptors. Thus, Z-338 is a gastrokinetic agent with a unique profile. ..
  46. Harris A, Cox S, Burns D, Norey C. Miniaturization of fluorescence polarization receptor-binding assays using CyDye-labeled ligands. J Biomol Screen. 2003;8:410-20 pubmed
    ..Z' factor values determined for the FP receptor assays in both 384- and 1536-well formats were found to be > 0.5, indicating the assays to be robust, reliable, and suitable for HTS purposes. ..
  47. Miller T, Zipursky R, Perkins D, Addington J, Woods S, Hawkins K, et al. The PRIME North America randomized double-blind clinical trial of olanzapine versus placebo in patients at risk of being prodromally symptomatic for psychosis. II. Baseline characteristics of the "prodromal" sample. Schizophr Res. 2003;61:19-30 pubmed
    ..Subsequent reports will detail the effects of drug versus placebo on prodromal symptoms, neuropsychological profile, and the rate of conversion to psychosis. ..
  48. Brunnauer A, Geiger E, Laux G. [Neuroleptics and cognition]. Psychiatr Prax. 2003;30 Suppl 2:S106-9 pubmed
    ..Results from this study suggest that even under clinical routine conditions atypical antipsychotics have an advantage on cognitive function when compared with conventional neuroleptics. ..
  49. Alcalá M, Maderuelo A, Vivas N, Camps P, Muñoz Torrero D, Clos M, et al. Effects of (+/-)-huprine Y and (+/-)-huprine Z, two new anticholinesterasic drugs, on muscarinic receptors. Neurosci Lett. 2005;379:106-9 pubmed
    ..Displacement of [3H]-pirenzepine and [3H]-QNB plus pirenzepine was performed in rat hippocampus...
  50. Fogl T, Margolese H. Fungal dermatitis with olanzapine in schizophrenia. Can J Psychiatry. 2003;48:643-4 pubmed
  51. Murakami Y, Zhao Q, Harada K, Tohda M, Watanabe H, Matsumoto K. Choto-san, a Kampo formula, improves chronic cerebral hypoperfusion-induced spatial learning deficit via stimulation of muscarinic M1 receptor. Pharmacol Biochem Behav. 2005;81:616-25 pubmed
    ..The effects of Choto-san and Uncaria were blocked by pirenzepine, a selective muscarinic M1 antagonist...
  52. Isaac M, Isaac M. Effect of divalproex combined with olanzapine or risperidone in patients with an acute exacerbation of schizophrenia. Neuropsychopharmacology. 2003;28:2049; author reply 2052-3 pubmed
  53. Lieberman J, Stroup T. Schizophrenia, VI: Treatments. Am J Psychiatry. 2003;160:1748 pubmed
  54. Marti M, Mevissen M, Althaus H, Steiner A. In vitro effects of bethanechol on equine gastrointestinal contractility and functional characterization of involved muscarinic receptor subtypes. J Vet Pharmacol Ther. 2005;28:565-74 pubmed
    ..The involvement of other muscarinic receptor subtypes cannot be excluded. Further studies are necessary to understand the effect of BeCh in vivo including diseased animals. ..
  55. Corya S, Andersen S, Detke H, Kelly L, Van Campen L, Sanger T, et al. Long-term antidepressant efficacy and safety of olanzapine/fluoxetine combination: a 76-week open-label study. J Clin Psychiatry. 2003;64:1349-56 pubmed
    ..The long-term safety profile of the combination was similar to that of its component monotherapies. ..
  56. Abramochkin D, Tapilina S, Sukhova G, Nikolsky E, Nurullin L. Functional M3 cholinoreceptors are present in pacemaker and working myocardium of murine heart. Pflugers Arch. 2012;463:523-9 pubmed publisher
    ..We conclude that M3 cholinoreceptors are present in pacemaker and working myocardium of murine heart, where they mediate negative cholinergic effects: slowing of sinus rhythm and shortening of action potentials. ..
  57. Nikolsky E, Vyskocil F, Bukharaeva E, Samigullin D, Magazanik L. Cholinergic regulation of the evoked quantal release at frog neuromuscular junction. J Physiol. 2004;560:77-88 pubmed
    ..The muscarinic agonists, oxotremorine and the propargyl ester of arecaidine, as well as antagonists such as pirenzepine, AF-DX 116 and methoctramine, alone or in combination, did not affect the dispersion of the release...
  58. Tsang S, Pomakian J, Marshall G, Vinters H, Cummings J, Chen C, et al. Disrupted muscarinic M1 receptor signaling correlates with loss of protein kinase C activity and glutamatergic deficit in Alzheimer's disease. Neurobiol Aging. 2007;28:1381-7 pubmed
  59. Wrzos H, Tandon T, Ouyang A. Mechanisms mediating cholinergic antral circular smooth muscle contraction in rats. World J Gastroenterol. 2004;10:3292-8 pubmed
    ..concentration-response curve was obtained after incubation of the muscle for 90 min with antagonists for M1 (pirenzepine), M2 (methoctramine) and M3 (darifenacin) muscarinic receptor subtypes...
  60. Sugawara Y, Echigo R, Kashima K, Minami H, Watanabe M, Nishikawa Y, et al. Intracellular calcium level is an important factor influencing ion channel modulations by PLC-coupled metabotropic receptors in hippocampal neurons. Brain Res. 2013;1512:9-21 pubmed publisher
    ..This current response was suppressed by pirenzepine (an M1-preferring antagonist), PLC inhibitor, non-selective cation channel blocker, and lowering [Ca(2+)]i...
  61. Jeon W, Gibbons A, Dean B. The use of a modified [3H]4-DAMP radioligand binding assay with increased selectivity for muscarinic M3 receptor shows that cortical CHRM3 levels are not altered in mood disorders. Prog Neuropsychopharmacol Biol Psychiatry. 2013;47:7-12 pubmed publisher
    ..Western blotting confirmed that CHRM3 protein levels were unchanged in these subjects. ..
  62. du Bois T, Bell W, Deng C, Huang X. A high n-6 polyunsaturated fatty acid diet reduces muscarinic M2/M4 receptor binding in the rat brain. J Chem Neuroanat. 2005;29:282-8 pubmed
    ..Using quantitative autoradiography, [(3)H]pirenzepine binding to muscarinic M1/M4 receptors and [(3)H]AF-DX384 binding to M2/M4 receptors were measured throughout ..
  63. Malina A, Gaskill J, McConaha C, Frank G, LaVia M, Scholar L, et al. Olanzapine treatment of anorexia nervosa: a retrospective study. Int J Eat Disord. 2003;33:234-7 pubmed
    ..These data lend support to the possibility that olanzapine may be useful in AN patients. A controlled trial is necessary to prove that olanzapine is efficacious. ..
  64. Dudel J. The time course of transmitter release in mouse motor nerve terminals is differentially affected by activation of muscarinic M1 or M2 receptors. Eur J Neurosci. 2007;26:2160-8 pubmed
    ..M2 receptors were activated with muscarine, while the M1 receptors were blocked by pirenzepine. M2 activation presented a slight, but highly significant augmentation of early releases...
  65. Takahashi Y, Kaba H. Muscarinic receptor type 1 (M1) stimulation, probably through KCNQ/Kv7 channel closure, increases spontaneous GABA release at the dendrodendritic synapse in the mouse accessory olfactory bulb. Brain Res. 2010;1339:26-40 pubmed publisher
    ..The carbachol effect was reduced by the muscarinic receptor type-1 and -4 (M1 and M4) antagonist pirenzepine (10 microM), but not by the M2 and M4 antagonist himbacine (10 microM)...
  66. Gur R, Kohler C, Ragland J, Siegel S, Bilker W, Loughead J, et al. Neurocognitive performance and clinical changes in olanzapine-treated patients with schizophrenia. Neuropsychopharmacology. 2003;28:2029-36 pubmed
    ..These results suggest that some effects of olanzapine may impact both symptoms and cognitive performance. ..
  67. Serebrova S. [The clinical effectiveness of rabeprazole in patients with acid-related gastric and duodenal diseases with various sensitivity of different types of parietal gastric cell receptors]. Klin Med (Mosk). 2007;85:61-4 pubmed
    ..Individual reception type was studied. The effects of pirenzepine and ranitidine (or famotidine) given in standard doses at the beginning of the week were studied in patients ..
  68. Opolka J, Rascati K, Brown C, Gibson P. Role of ethnicity in predicting antipsychotic medication adherence. Ann Pharmacother. 2003;37:625-30 pubmed
  69. Lakshmanan J, Oyachi N, Ahanya S, Liu G, Mazdak M, Ross M. Corticotropin-releasing factor inhibition of sheep fetal colonic contractility: mechanisms to prevent meconium passage in utero. Am J Obstet Gynecol. 2007;196:357.e1-7 pubmed
    ..In humans, fetal in utero meconium (MEC) passage rarely occurs before term gestation. We hypothesized the existence of inhibitory mechanism(s) preventing colonic motility and MEC passage prior to term...
  70. Giglio D, Andersson M, Aronsson P, Delbro D, Haraldsson B, Tobin G. Changes in muscarinic receptors in the toad urothelial cell line TBM-54 following acrolein treatment. Clin Exp Pharmacol Physiol. 2008;35:217-22 pubmed
    ..Pre-incubating cells with different muscarinic receptor antagonists (i.e. pirenzepine (M(1) receptor selective), methoctramine (M(2)/M(4) receptor selective) and 4-diphenylacetoxy-N-..
  71. Endoh T. Muscarinic M2 receptor inhibition of calcium current in rat nucleus tractus solitarius. Neuroreport. 2007;18:1141-5 pubmed
    ..These results indicate that ACh inhibits N-type and P/Q-type VDCCs via Gi-protein betagamma subunits mediated by M2 receptors in nucleus tractus solitarius. ..
  72. Garcia N, Santafe M, Salon I, Lanuza M, Tomas J. Expression of muscarinic acetylcholine receptors (M1-, M2-, M3- and M4-type) in the neuromuscular junction of the newborn and adult rat. Histol Histopathol. 2005;20:733-43 pubmed publisher
    ..of both newborn and adult rats, acetylcholine release was modified by the M1-receptor selective antagonists pirenzepine (10 microM) and MT-7 (100 nM) and by the M2-receptor selective antagonists methoctramine (1 microM) and AF-DX ..
  73. Wilson M, Gibson C, Hamm R. Haloperidol, but not olanzapine, impairs cognitive performance after traumatic brain injury in rats. Am J Phys Med Rehabil. 2003;82:871-9 pubmed
  74. Pesic S, Grbovic L, Stoiljkovic M, Nikolic V, Djokic J. Functional characterization of the muscarinic receptors involved in endothelium-dependent relaxation in isolated canine uterine artery. J Vet Pharmacol Ther. 2009;32:109-15 pubmed publisher
    ..Using a range of muscarinic receptor antagonists such as atropine (nonselective), pirenzepine (M(1)-selective), methoctramine (M(2)-selective) and p-fluoro-hexahydro-sila-difenidol (p-FHHSiD) (M(1)/M(3)) ..
  75. Davis M, Khawam E, Pozuelo L, Lagman R. Management of symptoms associated with advanced cancer: olanzapine and mirtazapine. A World Health Organization project. Expert Rev Anticancer Ther. 2002;2:365-76 pubmed
    ..The pharmacokinetics and pharmacodynamics of both agents are unique and explain many of the benefits. More research and clinical experience will be necessary to define their role in the palliation of advanced cancer. ..
  76. Sanchez Lemus E, Arias Montaño J. M1 muscarinic receptors contribute to, whereas M4 receptors inhibit, dopamine D1 receptor-induced [3H]-cyclic AMP accumulation in rat striatal slices. Neurochem Res. 2006;31:555-61 pubmed
    ..Taken together our results indicate that in addition to the inhibitory role of M(4) receptors, in rat striatum acetylcholine stimulates cAMP formation through the activation of M(1 )receptors and PKC stimulation. ..
  77. Kochhar S, Nwokike J, Jankowitz B, Sholevar E, Abed T, Baron D. Olanzapine overdose: a pediatric case report. J Child Adolesc Psychopharmacol. 2002;12:351-3 pubmed
    ..This paper reports a case of an olanzapine overdose in a 12-year-old boy. An opioid-like presentation was noted. Despite a high serum level of olanzapine, the patient made a complete recovery and showed no sequelae at follow-up. ..
  78. Dai S, Zeng J, Wang L. [Effect of pirenzepine on form deprivation myopia in chicks and its possible mechanism]. Zhonghua Yan Ke Za Zhi. 2006;42:42-7 pubmed
    To observe the effect of M1-selective muscarinic antagonist, pirenzepine, on form deprivation myopia and investigate the expression of MMP-2 and its inhibitor TIMP-2 in the fibrous sclera in order to better understand the mechanism by ..
  79. Scarr E, Sundram S, Keriakous D, Dean B. Altered hippocampal muscarinic M4, but not M1, receptor expression from subjects with schizophrenia. Biol Psychiatry. 2007;61:1161-70 pubmed
    Having shown a decrease in [3H]pirenzepine binding in the hippocampus from subjects with schizophrenia, we wished to determine whether such a change in radioligand binding was associated with changes in hippocampal mRNA for the ..
  80. Copeland L, Zeber J, Valenstein M, Blow F. Racial disparity in the use of atypical antipsychotic medications among veterans. Am J Psychiatry. 2003;160:1817-22 pubmed
    ..This may reflect concern over serious side effects, such as loss of white blood cells and fluctuations of serum glucose levels, or patient preference. ..
  81. Freudenmann R. [A case of delusional parasitosis in severe heart failure. Olanzapine within the framework of a multimodal therapy]. Nervenarzt. 2003;74:591-5 pubmed
    ..This case hints at (1) the effectiveness of olanzapine in DP and (2) the importance of general medical conditions in the therapeutic approach to DP. ..
  82. Meibach R. Comparative effectiveness of antipsychotic drugs. Am J Psychiatry. 2003;160:589-90; author reply 592-3 pubmed
  83. Wu W, Saunders R, Mishkin M, Turchi J. Differential effects of m1 and m2 receptor antagonists in perirhinal cortex on visual recognition memory in monkeys. Neurobiol Learn Mem. 2012;98:41-6 pubmed publisher
    ..in perirhinal cortex of muscarinic receptor subtypes, we locally infused either the m1-selective antagonist pirenzepine or the m2-selective antagonist methoctramine in animals performing one-trial visual recognition, and compared ..
  84. Love R, Kelly D. Olanzapine and risperidone. Am J Health Syst Pharm. 2003;60:487-8; author reply 488-9 pubmed
  85. Zefirov T, Ziyatdinova N, Zefirov A. Age-related peculiarities of inotropic response of rat myocardium to selective block of M1-cholinoreceptors. Bull Exp Biol Med. 2013;155:708-10 pubmed
    ..The inhibitory effect of pirenzepine on the contractile force of ventricular myocardium was revealed in 6-week rats.
  86. Bellgrove M, Vance A, Bradshaw J. Local-global processing in early-onset schizophrenia: evidence for an impairment in shifting the spatial scale of attention. Brain Cogn. 2003;51:48-65 pubmed
    ..These findings suggest an impaired ability to shift the spatial scale of attention from a global to a local spatial scale in early-onset schizophrenia. ..
  87. Hirota C, McKay D. M3 muscarinic receptor-deficient mice retain bethanechol-mediated intestinal ion transport and are more sensitive to colitis. Can J Physiol Pharmacol. 2006;84:1153-61 pubmed
    ..ISC responses to bethanechol were partially inhibited by pirenzepine in WT ileum, but not tetrodotoxin, suggesting involvement of a non-neuronal M1 muscarinic receptor...
  88. Gupta S, Steinmeyer C, Frank B, Madhusoodanan S, Lockwood K, Lentz B, et al. Hyperglycemia and hypertriglyceridemia in real world patients on antipsychotic therapy. Am J Ther. 2003;10:348-55 pubmed
    ..This finding suggests that the high prevalence of diabetes, lipid abnormalities, and hypertension in a young, chronically psychiatrically ill population makes the case for aggressive screening. ..
  89. Chengappa K, Baker R, Shao L, Yatham L, Tohen M, Gershon S, et al. Rates of response, euthymia and remission in two placebo-controlled olanzapine trials for bipolar mania. Bipolar Disord. 2003;5:1-5 pubmed
    ..Full remission is an important but potentially elusive goal during short-term management of acute mania. ..
  90. Scarr E, Cowie T, Kanellakis S, Sundram S, Pantelis C, Dean B. Decreased cortical muscarinic receptors define a subgroup of subjects with schizophrenia. Mol Psychiatry. 2009;14:1017-23 pubmed publisher
    ..We assessed cortical [(3)H]pirenzepine binding and sequenced the CHRM1 in 80 subjects with schizophrenia and 74 age sex-matched control subjects...