Search Results - "Thiesen, Louise"
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The CaMKIIα hub ligand Ph-HTBA promotes neuroprotection after focal ischemic stroke by a distinct molecular interaction
Published in Biomedicine & pharmacotherapy (01-12-2022)“…Ca2+/calmodulin-dependent protein kinase II alpha (CaMKIIα) is a potential target for acute neuroprotection due to its key role in physiological and…”
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In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1
Published in The Journal of pharmacology and experimental therapeutics (01-08-2015)“…γ-Hydroxybutyric acid (GHB) is a recreational drug, a clinically prescribed drug in narcolepsy and alcohol dependence, and an endogenous substance that binds…”
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Lack of evidence for synaptic high‐affinity γ‐hydroxybutyric acid (GHB) transport in rat brain synaptosomes and 11 Na+‐dependent SLC neurotransmitter transporters
Published in Journal of neurochemistry (01-04-2019)“…γ‐Hydroxybutyric acid (GHB) is an endogenous compound proposed to act as a neurotransmitter. Na+‐dependent, high‐affinity GHB transport has long been…”
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The γ-hydroxybutyric acid (GHB) analogue NCS-382 is a substrate for both monocarboxylate transporters subtypes 1 and 4
Published in European journal of pharmaceutical sciences (15-02-2020)“…The small-molecule ligand (E)-2-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[7]annulen-6-ylidene)acetic acid (NCS-382) is an analogue of γ-hydroxybutyric acid (GHB)…”
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GAT3 selective substrate l-isoserine upregulates GAT3 expression and increases functional recovery after a focal ischemic stroke in mice
Published in Journal of cerebral blood flow and metabolism (01-01-2019)“…Ischemic stroke triggers an elevation in tonic GABA inhibition that impairs the ability of the brain to form new structural and functional cortical circuits…”
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Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain
Published in Journal of medicinal chemistry (24-11-2022)“…Ca2+/calmodulin-dependent protein kinase II alpha (CaMKIIα) is a brain-relevant kinase and an emerging drug target for ischemic stroke and neurodegenerative…”
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Discovery and Optimization of 5‑Hydroxy-Diclofenac toward a New Class of Ligands with Nanomolar Affinity for the CaMKIIα Hub Domain
Published in Journal of medicinal chemistry (12-05-2022)“…The Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα) is a brain-relevant kinase involved in long-term potentiation and synaptic plasticity. We have…”
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Five-Membered N‑Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ‑Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters
Published in Journal of medicinal chemistry (27-06-2019)“…Given the heterogeneity within the γ-aminobutyric acid (GABA) receptor and transporter families, a detailed insight into the pharmacology is still relatively…”
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Pharmacological Characterization of [3H]ATPCA as a Substrate for Studying the Functional Role of the Betaine/GABA Transporter 1 and the Creatine Transporter
Published in ACS chemical neuroscience (21-03-2018)“…The betaine/γ-aminobutyric acid (GABA) transporter 1 (BGT1) is one of the four GABA transporters (GATs) involved in the termination of GABAergic…”
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Radiosynthesis and Evaluation of [11C]3-Hydroxycyclopent-1-enecarboxylic Acid as Potential PET Ligand for the High-Affinity γ‑Hydroxybutyric Acid Binding Sites
Published in ACS chemical neuroscience (18-01-2017)“…γ-Hydroxybutyric acid (GHB) is an endogenous neuroactive substance and proposed neurotransmitter with affinity for both low- and high-affinity binding sites. A…”
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