Taylor, Palmer Shyong, Yan-Jye Samskey, Nathan Ho, Kwok-Yiu Radic', Zoran Fenical, William Sharpless, K Barry Kovarik, Zrinka Camacho-Hernandez, Gisela-Andrea
Published in
Journal of neurochemistry
We detail here distinctive departures from lead classical cholinesterase re-activators, the pyridinium aldoximes, to achieve rapid CNS penetration and reactivation of AChE in the CNS (brain and spinal cord). Such reactivation is consistent with these non-canonical re-activators enhancing survival parameters in both mice and macaques following expos...
Matsuda, Kazuhiko
Published in
Pest management science
Neonicotinoids are selective modulators of insect nicotinic acetylcholine receptors (nAChRs). These widely deployed insecticides interact with the orthosteric sites of nAChRs, not only to activate nAChRs on their own, but also to block the desensitizing component of nAChR responses. To date recombinant vertebrate or insect/vertebrate hybrid nAChRs ...
Weggel, Loni A Pandya, Anshul A
Published in
Molecules (Basel, Switzerland)
Neuronal nicotinic acetylcholine receptors are cell membrane-bound ion channels that are widely distributed in the central nervous system. The α4β2 subtype of neuronal nicotinic acetylcholine receptor plays an important role in modulating the signaling pathways for pain. Previous studies have shown that agonists, partial agonists, and positive allo...
El Gayed, Ema Elhelbawy, R H Elhelbawy, N G
Published in
British journal of biomedical science
Deba, Farah Ramos, Kara Vannoy, Matthew Munoz, Kemburli Akinola, Lois S. Damaj, M. Imad Hamouda, Ayman K.
Published in
Molecules
Neuronal nicotinic acetylcholine receptor (nAChR)-based therapeutics are sought as a potential alternative strategy to opioids for pain management. In this study, we examine the antinociceptive effects of 3-(2-chlorophenyl)-5-(5-methyl-1-(piperidin-4-yl)-1 H -pyrazol-4-yl)isoxazole (CMPI), a novel positive allosteric modulator (PAM), with preferent...
Sun, Zhihua Zhangsun, Manqi Dong, Shuai Liu, Yiqiao Qian, Jiang Zhangsun, Dongting Luo, Sulan
Published in
Marine Drugs
Nicotinic acetylcholine receptors (nAChRs) are membrane receptors and play a major role in tumorigenesis and cancer progression. Here, we have investigated the differential expression of nAChR subunits in human breast cancer cell lines and breast epithelial cell lines at mRNA and protein levels and the effects of the αO-conotoxin GeXIVA, antagonist...
Otvos, Reka A Still, Kristina B M Somsen, Govert W Smit, August B Kool, Jeroen
Published in
SLAS discovery : advancing life sciences R & D
Natural extracts are complex mixtures that may be rich in useful bioactive compounds and therefore are attractive sources for new leads in drug discovery. This review describes drug discovery from natural products and in explaining this process puts the focus on ion-channel drug discovery. In particular, the identification of bioactives from natura...
Turner, Matthew W. Marquart, Leanna A. Phillips, Paul D. McDougal, Owen M.
Published in
Toxins
Nicotinic acetylcholine receptors (nAChRs) are found throughout the mammalian body and have been studied extensively because of their implication in a myriad of diseases. α-Conotoxins (α-CTxs) are peptide neurotoxins found in the venom of marine snails of genus Conus . α-CTxs are potent and selective antagonists for a variety of nAChR isoforms. Ove...
ludwig;, friedrich-alexander
Both enantiomers of [18F]flubatine are promising radioligands for neuroimaging of α4β2 nicotinic acetylcholine receptors (nAChRs) by positron emission tomography (PET). To support clinical studies in patients with early Alzheimer’s disease, a detailed examination of the metabolism in vitro and in vivo has been performed. (+)- and (−)-flubatine, res...
Oda, Akira Tanaka, Hidekazu
Published in
Neural regeneration research
The cholinergic system is involved in a broad spectrum of brain function, and its failure has been implicated in Alzheimer's disease. Acetylcholine transduces signals through muscarinic and nicotinic acetylcholine receptors, both of which influence synaptic plasticity and cognition. However, the mechanisms that relate the rapid gating of nicotinic ...
