Results 131 to 140 of about 177,108 (289)

Redox‐Activated Probes Enable High‐Contrast Live Imaging of Native Postsynaptic Scaffolds

Angewandte Chemie International Edition, EarlyView.
Sylives are modified fluorescent peptides for high‐contrast live imaging of inhibitory (gephyrin) and excitatory (PSD‐95) postsynaptic scaffolds in native neurons. Clean labeling requires low nanomolar probe levels, whereas uptake needs micromolar cell‐penetrating peptide (CPP).
Christiane Huhn, Clémence Mille, Sheng‐Yang Ho, Felix Lützenkirchen, Vladimir Khayenko, Melanie Hein, Christian Werner, Matthias Kneussel, Johannes W. Hell, Christian G. Specht, Hans M. Maric   +10 more
wiley   +1 more source

The Relationship Between Aldose Reductase and Isoxazole Derivatives: An In Vitro and In Silico Approach to Its Correlation With Diabetic Conditions

Biotechnology and Applied Biochemistry, EarlyView.
ABSTRACT Diabetes mellitus (DM), which can result in a number of problems such as cataracts, neuropathy, retinopathy, nephropathy, and several cardiovascular illnesses, continues to be a growing issue despite major advancements in treatment approaches.
Ahmet Esat Göner, Hatice Esra Duran
wiley   +1 more source

Safety and pharmacokinetics of a novel potent GABA analogue crisugabalin in Chinese subjects with various degrees of renal impairment

British Journal of Clinical Pharmacology, EarlyView.
Aims Crisugabalin is a novel calcium channel α2δ subunit ligand and a highly selective oral gamma‐aminobutyric acid (GABA) analogue developed for the treatment of diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). This study investigated pharmacokinetic properties and safety of crisugabalin in subjects with renal impairment ...
Shibeilei Lin, Ye Wang, Chao Hu, Yanhuan Feng, Xi Tang, Ping Fu, Jia Miao   +6 more
wiley   +1 more source

Hypnotic doses of fazamorexant induced less impairment on balance and cognition than zolpidem in healthy younger and elderly individualse

British Journal of Clinical Pharmacology, EarlyView.
Aims Fazamorexant is a dual orexin receptor antagonist being developed for the treatment of insomnia. This study aims to determine the dose‐exposure‐response relationship of single‐dose fazamorexant vs. zolpidem in young adult and elderly healthy Chinese volunteers. Methods This single‐centre, randomized, double‐blind, double‐dummy, placebo‐ and active‐
Chen Xia, Huang Xingxing, Jin Lu, Wang Ruwei   +3 more
wiley   +1 more source

Pathophysiological role of extrasynaptic GABAA receptors in typical absence epilepsy [PDF]

, 2011
GABA is the principal inhibitory neurotransmitter in the mammalian CNS. It acts via two classes of receptors, the GABAA, a ligand gated ion channel (ionotropic receptor) and the metabotropic G-protein coupled GABAB receptor.
Crunelli, Vincenzo, Di Giovanni, Giuseppe, Errington, Adam C.   +2 more
core  

Cannabinoids and drug–drug pharmacokinetic interactions: Deciphering the risks

British Journal of Clinical Pharmacology, EarlyView.
The relationship between cannabinoids and mental health has become a major focus of scientific inquiry and public discourse. Cannabinoids are diverse chemical compounds from the Cannabis species that have been explored for their therapeutic applications in treating chronic pain, psychiatric and neurological conditions, such as depression, schizophrenia,
Paraskevi Papakyriakopoulou, Georgia Valsami, Georgios Ismailos   +2 more
wiley   +1 more source

Establishing an Ion Pair Interaction in the Homomeric {rho}1 {gamma}-Aminobutyric Acid Type A Receptor That Contributes to the Gating Pathway [PDF]

, 2007
{gamma}-Aminobutyric acid type A (GABAA) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. Upon agonist binding, the receptor undergoes a structural transition from the closed to the open state, but the mechanism of gating ...
Dougherty, Dennis A., Lester, Henry A., Wang, Jinti   +2 more
core  

Zuranolone: A case study in (regulatory) rush to judgement?

British Journal of Clinical Pharmacology, EarlyView.
Abstract Sage, in collaboration with Biogen, submitted a new drug approval for zuranolone for postpartum depression (PPD) and major depressive disorder (MDD) in December 2022. In August 2023, the US Food and Drug Administration granted approval for PPD but denied approval for MDD.
Lisa Cosgrove, Milutin Kostic, Barbara Mintzes, Gianna D'Ambrozio, Allen Shaughnessy   +4 more
wiley   +1 more source

Rubrolides A, D, P, T, U: Total Syntheses and Antibacterial Evaluation of Highly Brominated Marine Natural Products

ChemistryEurope, EarlyView.
Following the Danube Flow. The first total syntheses of highly brominated rubrolides T, U, and U‐analog, together with the efficient and divergent syntheses of rubrolides A, D, and P. The dibrominated key intermediate, obtained via a Suzuki‐Miyaura cross‐coupling reaction, is the centerpiece of the synthesis.
Jasmin Janneschütz, Paul G. Schebek, Alexander Meyer, Celina Haller, Sophia Khom, Wolfgang R. Streit, Ifey Alio, Nina Schützenmeister   +7 more
wiley   +1 more source

Structural studies of human GABA-A receptors

, 2017
Type-A γ-amino-butyric acid receptors (GABAARs) are pentameric ligand-gated ion channels (pLGICs), which mediate the majority of fast inhibitory neurotransmission in the animal central nervous system. Their dysfunction is related to numerous conditions including epilepsy, insomnia, anxiety, panic disorders, depression and schizophrenia.
openaire   +2 more sources