From 2-triethylammonium ethyl ether of 4-stilbenol (MG624) to selective small-molecule antagonists of human α9α10 nicotinic receptor by modifications at the …
F Bavo, M Pallavicini, S Pucci, R Appiani… - Journal of medicinal …, 2022 - ACS Publications
Nicotinic acetylcholine receptors containing α9 subunits (α9*-nAChRs) are potential
druggable targets arousing great interest for pain treatment alternative to opioids …
druggable targets arousing great interest for pain treatment alternative to opioids …
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic …
G Zheng, Z Zhang, C Dowell, E Wala… - Bioorganic & medicinal …, 2011 - Elsevier
A series of azaaromatic quaternary ammonium analogs has been discovered as potent and
selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary …
selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary …
Subnanomolar affinity and selective antagonism at α7 nicotinic receptor by combined modifications of 2-triethylammonium ethyl ether of 4-Stilbenol (MG624)
F Bavo, M Pallavicini, S Pucci, R Appiani… - Journal of Medicinal …, 2022 - ACS Publications
Modifications of the cationic head and the ethylene linker of 2-(triethylammonium) ethyl ether
of 4-stilbenol (MG624) have been proved to produce selective α9*-nAChR antagonism …
of 4-stilbenol (MG624) have been proved to produce selective α9*-nAChR antagonism …
[HTML][HTML] Small molecule ligands for α9* and α7 nicotinic receptors: A survey and an update, respectively
A Giraudo, M Pallavicini, C Bolchi - Pharmacological Research, 2023 - Elsevier
Abstract The α9-and α7-containing nicotinic acetylcholine receptors (nAChRs) mediate
numerous physiological and pathological processes by complex mechanisms that are …
numerous physiological and pathological processes by complex mechanisms that are …
Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic …
H Andleeb, RL Papke, C Stokes, K Richter… - Journal of Medicinal …, 2024 - ACS Publications
There is an urgent need for nonopioid treatments for chronic and neuropathic pain to
provide effective alternatives amid the escalating opioid crisis. This study introduces novel …
provide effective alternatives amid the escalating opioid crisis. This study introduces novel …
2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands
A Mazurov, J Klucik, L Miao, TY Phillips… - Bioorganic & Medicinal …, 2005 - Elsevier
A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as α7 neuronal
nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore …
nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore …
Discovery and development of α7 nicotinic acetylcholine receptor modulators
AA Mazurov, JD Speake… - Journal of medicinal …, 2011 - ACS Publications
Efforts in the design and discovery of selective α7 nicotinic acetylcholine receptor (nAChR)
agonists were both facilitated and hampered by observation that ligands can show dual …
agonists were both facilitated and hampered by observation that ligands can show dual …
Activation and inhibition of the human α7 nicotinic acetylcholine receptor by agonists
CA Briggs, DG McKenna - Neuropharmacology, 1998 - Elsevier
To better understand the effects of weak as well as strong agonists at the human α7 nicotinic
acetylcholine receptor (human α7 nAChR), the abilities of several classic nAChR agonists to …
acetylcholine receptor (human α7 nAChR), the abilities of several classic nAChR agonists to …
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333
C Beinat, SD Banister, S van Prehn… - Bioorganic & medicinal …, 2012 - Elsevier
A series of ligands based on SEN12333, containing either contracted or elongated alkyl
chains, were synthesized and evaluated in molecular docking studies against a homology …
chains, were synthesized and evaluated in molecular docking studies against a homology …
Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor
K Chojnacka, RL Papke, NA Horenstein - Bioorganic & medicinal chemistry …, 2013 - Elsevier
We introduce the term 'silent agonists' to describe ligands that can place the α7 nicotinic
acetylcholine receptor (nAChR) into a desensitized state with little or no apparent activation …
acetylcholine receptor (nAChR) into a desensitized state with little or no apparent activation …
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