Results 91 to 100 of about 493,465 (339)

Spirocyclic Diamine Scaffolds for Medicinal Chemistry

Helvetica Chimica Acta, EarlyView.
Here we enumerated 391 spirocyclic diamine drug scaffolds with ring sizes four to eight and found that most of them are unknown. We prepared four novel such spirocycles and discovered a micromolar inhibitor of the M4 muscarinic receptor. ABSTRACT Medicinal chemistry requires the exploration of structurally diverse compound families to expand the ...
Aline Carrel, Alejandro Flores, Maedeh Darsaraee, Jean‐Louis Reymond   +3 more
wiley   +1 more source

High Throughput Random Mutagenesis and Single Molecule Real Time Sequencing of the Muscle Nicotinic Acetylcholine Receptor. [PDF]

PLoS ONE, 2016
High throughput random mutagenesis is a powerful tool to identify which residues are important for the function of a protein, and gain insight into its structure-function relation.
Paul J Groot-Kormelink, Sandrine Ferrand, Nicholas Kelley, Anke Bill, Felix Freuler, Pierre-Eloi Imbert, Anthony Marelli, Nicole Gerwin, Lucia G Sivilotti, Loren Miraglia, Anthony P Orth, Edward J Oakeley, Ulrich Schopfer, Sandra Siehler   +13 more
doaj   +1 more source

Mechanisms of spinal glial activation in chemotherapy‐induced peripheral neuropathy: Focus on microglia and astrocytes

Ibrain, EarlyView.
Chemotherapy‐induced peripheral neuropathy (CIPN) remains a major clinical challenge, with central sensitization considered an important pathological mechanism in its occurrence and persistence. This review focuses on spinal astrocytes and microglia, systematically summarizing the pathological mechanisms of spinal glial cells involved in CIPN caused by
Long Gu, Song Cao, Yonghuai Feng
wiley   +1 more source

Defining nicotinic agonist binding surfaces through photoaffinity labeling.

Biochemistry, 2007
Nicotinic acetylcholine (ACh) receptor (nAChR) agonists are potential therapeutic agents for neurological dysfunction. In the present study, the homopentameric mollusk ACh binding protein (AChBP), used as a surrogate for the extracellular ligand-binding ...
M. Tomizawa, D. Maltby, K. Medzihradszky, Nanjing Zhang, K. A. Durkin, J. Presley, T. Talley, P. Taylor, A. Burlingame, J. Casida   +9 more
semanticscholar   +1 more source

Molecular imprinting for neurology: Materials, applications, and limitations

Ibrain, EarlyView.
Molecularly imprinted materials: diagnostic, therapeutic and research applications in neurology. Molecularly imprinted materials offer high specificity and affinity for target molecules in neurological applications. This review highlights their synthesis, characterisation, and use in diagnostics, research and therapeutics.
Xiaohan Ma, Yingqi Ma, Claudia Marino, Alessandro Poma   +3 more
wiley   +1 more source

Minimal Structural Changes Determine Full and Partial Nicotinic Receptor Agonist Activity for Nicotine Analogues

Molecules, 2019
Neuronal α4β2 nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels (LGIC) that have been implicated in nicotine addiction, reward, cognition, pain disorders, anxiety, and depression.
Juan Pablo Gonzalez-Gutierrez, Martin Hodar, Franco Viscarra, Pablo Paillali, Nicolás Guerra-Díaz, Hernán Pessoa-Mahana, Juan José Hernández-Morantes, Horacio Pérez-Sánchez, Isabel Bermúdez, Miguel Reyes-Parada, Patricio Iturriaga-Vásquez   +10 more
doaj   +1 more source

Pharmacological MRI: Utility in Understanding Drug Mechanisms in Psychiatric Disorders

Journal of Magnetic Resonance Imaging, EarlyView.
ABSTRACT Pharmacological MRI (pharmaMRI) has emerged as a powerful tool to study how psychoactive drugs affect brain function and to uncover mechanisms of drug action in psychiatric disorders. This review provides an overview of key techniques used in pharmaMRI, including BOLD‐fMRI, arterial spin labeling (ASL), and cerebral blood volume (CBV) mapping,
Christin Y. Sander, Tudor M. Ionescu, Mitul A. Mehta, Ottavia Dipasquale, Anouk Schrantee   +4 more
wiley   +1 more source

Varenicline Ameliorates Learning and Memory Deficits in Amyloid β(25–35) Rat Model of Alzheimer’s Disease

Basic and Clinical Neuroscience, 2011
Introduction: Alzheimer’s disease (AD) is a enfeeble neurodegenerative disorder characterized by increased β-amyloid (Aβ) deposition and neuronal dysfunction leading to impaired learning and recall.
Tourandokht Baluchnejadmojarad, Mehrdad Roghani, Narges karimi, Mitra kamran   +3 more
doaj  

Two Amino Acid Residues Contribute to a Cation-π Binding Interaction in the Binding Site of an Insect GABA Receptor [PDF]

, 2011
Cys-loop receptor binding sites characteristically possess an "aromatic box," where several aromatic amino acid residues surround the bound ligand. A cation-π interaction between one of these residues and the natural agonist is common, although the ...
Ashby, Jamie A., Dougherty, Dennis A., Lummis, Sarah C. R., McGonigle, Ian   +3 more
core  

Intracellular mechanisms underlying the nicotinic enhancement of LTP in the rat dentate gyrus [PDF]

, 2008
We have previously shown that activation of nicotinic acetylcholine receptors (nAChRs) enhanced long-term potentiation (LTP) in the rat dentate gyrus in vitro via activation of α7 nAChR. In the present studies, mechanisms underlying the acute and chronic
Abel, Arendt, Atack, Bain, Bear, Blanquet, Bliss, Blitzer, Blitzer, Bogan, Casey, Charpantier, Cho, Dajas-Bailador, Davies, Davis, Decker, Dhavan, Dominguez del Toro, English, Faghih, Fujii, Giovannini, Gray, Hope, Huang, Huang, Hunter, Hurst, Ji, Jones, Kawakami, Kelly, Kihara, Klein, Krause, Le Novere, Levin, Li, Liston, Lu, Man, Mann, Marrero, Matsuyama, Matthies, Meriane, Opazo, O’Dell, Peavy, Picciotto, Polesskaya, Polesskaya, Radcliffe, Roberson, Rush, Salazar, Sanna, Sanna, Santos, Seguela, Sharifzadeh, Sharifzadeh, Sharma, Shaw, Shaw, Sweatt, Takada-Takatori, Tominaga-Yoshino, Wada, Wang, Wang, Welsby, Welsby, Whitehouse, Woo, Wu, Yang, Ying, Yu, Zhang, Zwart   +81 more
core   +1 more source