Update Opipramol

Gahr, Maximilian; Hiemke, Christoph; Connemann, Bernhard J.

doi:10.1055/s-0043-100762

Cited by 16 publications

(5 citation statements)

References 17 publications

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“…Opipramol diHCl (OPI): OPI was developed originally as an antidepressant and later used as a treatment for somatoform disorder ( Gahr et al, 2017 ). The sigma receptor agonist did not affect HR in myl7:eGFP or change HS ( Figure 4A ).…”

Section: Resultsmentioning

confidence: 99%

“…Nevertheless, DLX dose-dependently increased the ToxScore, resulting in complete lethality at 80 µM (Figure 6C). Opipramol diHCl (OPI): OPI was developed originally as an antidepressant and later used as a treatment for somatoform disorder (Gahr et al, 2017). The sigma receptor agonist did not affect HR in myl7:eGFP or change HS (Figure 4A).…”

Section: Pyrvinium Pamoate (Pp)mentioning

confidence: 99%

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pyHeart4Fish: Chamber-specific heart phenotype quantification of zebrafish in high-content screens

Vedder¹,

Reinberger²,

Haider³

et al. 2023

Front. Cell Dev. Biol.

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Cardiovascular diseases (CVDs) are the leading cause of death. Of CVDs, congenital heart diseases are the most common congenital defects, with a prevalence of 1 in 100 live births. Despite the widespread knowledge that prenatal and postnatal drug exposure can lead to congenital abnormalities, the developmental toxicity of many FDA-approved drugs is rarely investigated. Therefore, to improve our understanding of drug side effects, we performed a high-content drug screen of 1,280 compounds using zebrafish as a model for cardiovascular analyses. Zebrafish are a well-established model for CVDs and developmental toxicity. However, flexible open-access tools to quantify cardiac phenotypes are lacking. Here, we provide pyHeart4Fish, a novel Python-based, platform-independent tool with a graphical user interface for automated quantification of cardiac chamber-specific parameters, such as heart rate (HR), contractility, arrhythmia score, and conduction score. In our study, about 10.5% of the tested drugs significantly affected HR at a concentration of 20 µM in zebrafish embryos at 2 days post-fertilization. Further, we provide insights into the effects of 13 compounds on the developing embryo, including the teratogenic effects of the steroid pregnenolone. In addition, analysis with pyHeart4Fish revealed multiple contractility defects induced by seven compounds. We also found implications for arrhythmias, such as atrioventricular block caused by chloropyramine HCl, as well as (R)-duloxetine HCl-induced atrial flutter. Taken together, our study presents a novel open-access tool for heart analysis and new data on potentially cardiotoxic compounds.

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Section: Resultsmentioning

confidence: 99%

Section: Pyrvinium Pamoate (Pp)mentioning

confidence: 99%

pyHeart4Fish: Chamber-specific heart phenotype quantification of zebrafish in high-content screens

Vedder¹,

Reinberger²,

Haider³

et al. 2023

Front. Cell Dev. Biol.

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“…Vielmehr wirkt Opipramol hauptsächlich durch eine Bindung an σ-Rezeptoren mit der Folge einer Modulation im NMDA-System (NMDA: N-Methyl-D-Aspartat). Aufgrund der vor allem anxiolytischen sowie sedierenden Wirkung kommt Opipramol häufig zur Behandlung von Angsterkrankungen, Unruhe und Schlafstörungen und eher seltener zur antidepressiven Therapie zur Anwendung [5,13,14]. [16].…”

Section: Opipramolunclassified

Perioperatives Management psychiatrischer und neurologischer Dauermedikation

Bischoff¹,

Redel²

2021

Anästhesiol Intensivmed Notfallmed Schmerzther

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ZusammenfassungEtwa ein Drittel aller Patienten, die sich einem operativen Eingriff unterziehen, nehmen chronisch Psychopharmaka ein. Neben Depressionen und Psychosen stellen chronische Schmerzen sowie Angst- und Panikstörungen die häufigsten Indikationen dar. In den vergangenen 30 Jahren stieg die Häufigkeit der Verordnung von Psychopharmaka um das 7-Fache. Fast alle Psychopharmaka interagieren mit Medikamenten, die perioperativ häufig gegeben werden, beispielsweise mit 5-HT3-Antagonisten, Sympathomimetika oder Opioiden. Einige der Medikamente weisen eine enge therapeutische Breite auf und nicht alle Medikamente können perioperativ pausiert werden. Im Rahmen der präoperativen Risikoevaluation ist daher eine Prüfung im Einzelfall notwendig. Der Anästhesist muss zudem bei Gabe bestimmter Medikamente während der Narkose besondere Vorsicht walten lassen oder ganz auf diese verzichten.Bei der Therapie vieler neurologischer Erkrankungen stellen Medikamente die zentrale Säule dar. Häufig begegnen dem Anästhesisten Patienten mit einer Epilepsie, mit Morbus Parkinson oder mit einer Myasthenia gravis, die eine entsprechende medikamentöse Therapie erhalten. Das perioperative Pausieren der Medikamente lässt zumeist eine Befundverschlechterung der neurologischen Grunderkrankung befürchten. Auf die möglichst rasche postoperative Einnahme der Dauermedikation ist daher besonderer Wert zu legen.

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“…Opipramol (IS-opi) is a member of tricyclic antidepressants (TCAs) [Korobkova et al 2010] and was developed in the 1960s (Gahr et al 2017). Typically used in the treatment of generalized anxiety disorder (GAD) and somatoform disorders.…”

Section: Introductionmentioning

confidence: 99%

“…Most TCAs act as monoamine reuptake inhibitors, but opipramol does not, and instead acts primarily as a sigma receptor agonist. It was reported that opipramol was metabolized by P450 2D6 (Gillman 2007;Gahr et al 2017). In plasma and urine was identified oxidation product of the hydroxyethyl moiety to an acetic acid group at the piperazine side chain, decarboxylation products, opipramol-N-oxide, deshydroxyethyl metabolite, and dibenzoazepine.…”

Section: Introductionmentioning

confidence: 99%

Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes

et al. 2021

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The present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase II, including UGT, often creates problems in correct selection of valuable compounds. Moreover, microsomes data set is richer in the contest and provides medical scientist to determine also the susceptibility of drugs to undergo phase I and then phase II. In the present work, we have shown that IS-noh was metabolized in vitro by phase I enzymes to the oxidation product, which was next transformed with UGTs to glucuronide. The results showed also that the previously known oxidation product of opipramol was changed to previously no reported glucuronidation product by UDP-glucuronosyltransferases. In addition, unlike IS-noh, opipramol did not prove to be the substrate for UGTs. Therefore, tricyclic antidepressants depending on the structure can trigger a different response after contact with UGT enzymes. Some will metabolize directly with UGTs, others only after activation by phase I enzymes.

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Update Opipramol

Cited by 16 publications

References 17 publications

pyHeart4Fish: Chamber-specific heart phenotype quantification of zebrafish in high-content screens

pyHeart4Fish: Chamber-specific heart phenotype quantification of zebrafish in high-content screens

Perioperatives Management psychiatrischer und neurologischer Dauermedikation

Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes

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