Article
Pharmacology & Pharmacy
Roger L. Papke, Marta Quadri, Alican Gulsevin
Summary: We discuss models for the activation and desensitization of alpha 7 nicotinic acetylcholine receptors (nAChRs), as well as the effects of type II positive allosteric modulators (PAMs) that destabilize alpha 7 desensitized states. The cholinergic anti-inflammatory system (CAS) modulates inflammation and pain through alpha 7 nAChRs in cells of the immune system. Silent agonists and type II PAMs play important roles in CAS regulation.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Nicole A. Horenstein, Clare Stokes, Roger L. Papke
Summary: The study suggests that various sulfonium compounds can be used to desensitize the alpha 7 receptor, with 4-hydroxyphenyldimethylsulfonium and suplatast sulfonium salts being the most effective desensitizers. Additionally, it was found that the smallest sulfonium compound, trimethylsulfonium, acts as a partial agonist for alpha 7 and other neuronal nAChR. The results indicate that these compounds may be valuable for further development of alpha 7 desensitizing ability and receptor subtype selectivity.
Article
Neurosciences
Xiao-Tao Jin, Ryan M. Drenan
Summary: The interpeduncular nucleus (IPN) is involved in nicotine dependence and regulation of fear responses, affective states, and novelty processing. Neurons in the IPN express nicotinic acetylcholine receptors (nAChR) and receive cholinergic innervation. Studies have shown that IPL neurons express Chrna7 (alpha 7 nAChR subunit) and are sensitive to acetylcholine (ACh) stimulation. These findings contribute to a better understanding of cholinergic modulation in the IPN.
Review
Biochemistry & Molecular Biology
Virginia Borroni, Francisco J. Barrantes
Summary: Nicotinic acetylcholine receptors (nAChRs) play a crucial role in neurotransmission and cell signaling, with different types of nAChR pentamers having distinct effects on brain function. Due to its central role in various fundamental brain processes, α7 nAChR is associated with numerous neurological and neuropsychiatric disorders.
Review
Biochemistry & Molecular Biology
Bowen Jia, Jing Li, Yiting Song, Chengliang Luo
Summary: Ferroptosis is a form of iron-dependent regulated cell death characterized by iron-dependent lipid peroxidation and has been implicated in various diseases, including nervous system diseases and injuries. ACSL4, a member of the ACSLs family, is involved in the regulation of arachidonic acid and eicosapentaenoic acid, leading to ferroptosis. Understanding the molecular mechanisms of ACSL4-mediated ferroptosis will contribute to the development of new treatment strategies for these diseases or injuries.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Juan Facundo Chrestia, Maria del Carmen Esandi, Cecilia Bouzat
Summary: Cannabidiol (CBD), a terpenoid compound from marijuana, has attracted pharmaceutical interest for its potential therapeutic uses. This study reveals the molecular mechanisms by which CBD modulates the function of the alpha 7 nicotinic acetylcholine receptor (alpha 7 nAChR), which is involved in various pathological conditions. CBD inhibits alpha 7 nAChR activity and decreases intracellular calcium responses, providing insights into its pharmacological relevance.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2022)
Article
Clinical Neurology
Ari Dienel, Remya A. Veettil, Kanako Matsumura, Jude P. J. Savarraj, H. Alex Choi, Peeyush T. Kumar, Jaroslaw Aronowski, Pramod Dash, Spiros L. Blackburn, Devin W. McBride
Summary: The study demonstrates that stimulating nicotinic acetylcholine alpha(7) receptors (α(7)-AChR) can reduce inflammation and improve outcomes in aneurysmal subarachnoid hemorrhage. Animal experiments and analysis of patient plasma samples support α(7)-AChR as a potential target for treating SAH.
Review
Neurosciences
Maria Rosaria Tropea, Domenica D. Li Puma, Marcello Melone, Walter Gulisano, Ottavio Arancio, Claudio Grassi, Fiorenzo Conti, Daniela Puzzo
Summary: The deletion of alpha 7nAChR leads to impaired hippocampal synaptic plasticity and memory, along with an increase in Amyloid Precursor Protein expression and A beta levels, resembling classic features of Alzheimer's disease (AD).
PROGRESS IN NEUROBIOLOGY
(2021)
Review
Oncology
Zhe-Qi Xu, Wen-Jun Zhang, Ding-Feng Su, Guo-Qing Zhang, Chao-Yu Miao
Summary: The ?7 nicotinic acetylcholine receptor has widespread expression in the central nervous system and its activation leads to various physiological processes with different cellular responses. The research has shown contradictory phenomena that require further studies for clarification.
ANNALS OF TRANSLATIONAL MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Alessandro Giraudo, Marco Pallavicini, Cristiano Bolchi
Summary: The alpha 9- and alpha 7-containing nicotinic acetylcholine receptors play key roles in physiological and pathological processes. Selective ligands for these receptors are important research tools and potential therapeutic agents. While there is a wealth of information on alpha 7-nAChR ligands, the understanding of selective alpha 9-nAChR ligands is limited. This review provides a comprehensive overview of the latter, along with recent updates on alpha 7-nAChR ligands.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Cell Biology
Yuan Liu, Shi Xu, Haijun Zhang, Kaoliang Qian, Jiachen Huang, Xianger Gu, Yan Li, Yi Fan, Jun Hu
Summary: OA patients showed decreased levels of alpha 7-nAChRs and an imbalance between autophagy and apoptosis in knee joint cartilage tissues.
CELL DEATH & DISEASE
(2021)
Article
Pharmacology & Pharmacy
Victoria R. Sanders, Neil S. Millar
Summary: Considerable progress has been made in the identification and characterization of subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs), specifically alpha 7 nAChRs. This review focuses on alpha 7-selective modulators that bind to receptor sites other than the orthosteric agonist binding site for acetylcholine. The mechanism of action and binding sites of these modulators is still a topic of debate.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Neurosciences
Ari Dienel, Remya A. Veettil, Kanako Matsumura, H. Alex Choi, Peeyush T. Kumar, Andrey S. Tsvetkov, Jaroslaw Aronowski, Pramod Dash, Spiros L. Blackburn, Devin W. McBride
Summary: Stimulation of alpha 7-AChR promotes neuronal survival and improves neurobehavioral outcomes after SAH, with increased PI3K/Akt activity playing a key role in mediating these effects. Knockout studies and cell culture experiments support a direct effect of alpha 7-AChR agonism on promoting cell survival.
EXPERIMENTAL NEUROLOGY
(2021)
Review
Biochemistry & Molecular Biology
Tehila Mizrachi, Adi Vaknin-Dembinsky, Talma Brenner, Millet Treinin
Summary: This review discusses the role of nicotinic acetylcholine receptors in immune cell function and neurodegenerative diseases, as well as the therapeutic implications of activating the cholinergic anti-inflammatory pathway for diseases involving neuroinflammation.
Article
Biochemistry & Molecular Biology
Qimeng Li, Akos Nemecz, Gabriel Ayme, Gabrielle Dejean de la Batie, Marie S. Prevost, Stephanie Pons, Nathalie Barilone, Rayen Baachaoui, Uwe Maskos, Pierre Lafaye, Pierre-Jean Corringer
Summary: Two single-domain antibody fragments, C4 and E3, have been found to bind to the α7-nAChR and have different functional properties, indicating the importance of the extracellular site.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2023)
