Petra Scholze

Development of Novel Pegylated Imidazobenzodiazepines Targeting α5 GABAA Receptors for Anxiety: A Comparative Prodrug and Metabolite Study

Mubaraq A. Toriola, Ethan T Kowalczyk, Kayode M. Medubi, Michelle J. Meyer et autres

We report on the development of a highly water-soluble pegylated imidazodiazepine ETK-II-83. The compound binds selectively to GABAA receptors among forty-five other receptors expressed in the brain with a higher affinity for the α5-containing GABAA receptors. The compound is converted in vitro …

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A uniform tissue-clearing framework and mesoSPIM-ultra enable cm-scale single-neuron tracing

Marko Pende, Jared M. Cregg, Saiedeh Saghafi, Samuel Broadbent et autres

Summary Tissue-clearing and light-sheet microscopy have transformed volumetric imaging of intact organs, yet limited mechanistic understanding of dehydration-based clearing continues to constrain rational protocol design and broader applicability. Here, we define the cardinal chemical and physical principles underlying dehydration-based tissue-clearing and establish …

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Nezavist (DCUK-OEt) and aminoquinoline analogues interact with the etomidate site and display a complex mode of modulatory action of the GABAA receptor

Xenia Simeone, Sophia Khom, Angelika Maria Doppler, Thomas Seidel et autres

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Plasticity of ventral tegmental area disturbance during abstinence after repeated amphetamine exposure: restoration by selective activation of group II metabotropic glutamate receptors

Ornella Valenti, Katarzyna Anna Rekawek, Sophie Wieser, Petra Scholze et autres

Background and aims: The psychostimulant actions of amphetamine (AMPH) have been correlated with its ability to orchestrate ventral tegmental area (VTA) dopamine (DA) neuron activity states and, thus, DA release in output regions: in rats, a single exposure is sufficient to reduce …

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α7‐Nicotinic Acetylcholine Receptor and Mutated α‐Synuclein Interact in Motor Behaviour and Nigrostriatal Dopamine—Findings With Potential Relevance for a Protective Effect of Cigarette Smoking and Parkinson's Disease

Christian Pifl, Alexandra Wolf, Mark Elevado, Petra Scholze

Parkinson's disease (PD) occurs less frequently in cigarette smokers than in nonsmokers. Assuming that nicotinic acetylcholine receptors are periodically active by activation through endogenous acetylcholine, we tested whether they act against the effect of α-synuclein, a protein relevant in PD. Transgenic mice …

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Author response for "α7-Nicotinic Acetylcholine Receptor and Mutated α-Synuclein Interact in Motor Behaviour and Nigrostriatal Dopamine-Findings With Potential Relevance for a Protective Effect of Cigarette Smoking and Parkinson's Disease"

Christian Pifl, Alexandra Wolf, Mark Elevado, Petra Scholze

α7-nicotinic acetylcholine receptor and mutated α-synuclein interact in motor behavior and nigrostriatal dopamine - findings with potential relevance for a protective effect of cigarette smoking and Parkinson’s disease

Christian Pifl, Alexandra Wolf, Mark Elevado, Petra Scholze

Parkinson’s disease (PD) occurs less frequently in cigarette smokers than in non-smokers. Assuming that nicotinic acetylcholine receptors are periodically active by activation through endogenous acetylcholine, we tested whether they act against the effect of α-synuclein, a protein relevant in PD. Transgenic mice …

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The human‐specific nicotinic receptor subunit CHRFAM7A reduces α7 receptor function in human induced pluripotent stem cells‐derived and transgenic mouse neurons

Ilayda Görgülü, Vinita Jagannath, Stéphanie Pons, Filip Koniuszewski et autres

We investigated the impact of the human-specific gene CHRFAM7A on the function of α7 nicotinic acetylcholine receptors (α7 nAChRs) in two different types of neurons: human-induced pluripotent stem cell (hiPSC)-derived cortical neurons, and superior cervical ganglion (SCG) neurons, taken from transgenic mice …

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The human-specific nicotinic receptor subunit CHRFAM7A reduces α7 nAChR function in human iPSC-derived and transgenic mouse neurons

Ilayda Görgülü, Vinita Jagannath, Stéphanie Pons, Filip Koniuszewski et autres

We investigated the impact of the human-specific protein CHRFAM7A (also referred to as “dupα7”) on the function of α7 nicotinic acetylcholine receptors (nAChRs) in two different types of neurons: human induced pluripotent stem cell (hiPSC)-derived cortical neurons, and superior cervical ganglion (SCG) …

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Author response for "The human‐specific nicotinic receptor subunit CHRFAM7A reduces α7 receptor function in human induced pluripotent stem cells‐derived and transgenic mouse neurons"

Ilayda Görgülü, Vinita Jagannath, Stéphanie Pons, Filip Koniuszewski et autres

Probes for the heterogeneity of muscimol binding sites in rat brain

Veronika I. Müller, Margot Ernst, Aygul Baykuchkarova, Filip Koniuszewski et autres

Introduction: The plant-based alkaloid muscimol is a potent agonist of inhibitory GABAA-neurotransmitter receptors. GABAA receptors are a heterogeneous family of pentameric complexes, with 5 out of 19 subunits assembling around the central anion pore. Muscimol is considered to bind to all receptor …

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New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy

Dishary Sharmin, Branka Divović, Xingjie Ping, Rok Cerne et autres

KRM-II-81 (1) is an imidazodiazepine GABA A receptor (GABAAR) potentiator with broad antiseizure efficacy and a low sedative burden. A brominated analogue, DS-II-73 (5), was synthesized and pharmacologically characterized as a potential backup compound as KRM-II-81 moves forward into development. The synthesis …

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