scholarly journals Differentiation of the open and closed states of the ionic channels of nicotinic acetylcholine receptors by tricyclic antidepressants.

1981 ◽  
Vol 78 (8) ◽  
pp. 5240-5244 ◽  
Author(s):  
G. G. Schofield ◽  
B. Witkop ◽  
J. E. Warnick ◽  
E. X. Albuquerque
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Tricyclic Antidepressants ◽  
Ionic Channels ◽  
Nicotinic Acetylcholine

Tricyclic antidepressants inhibit hippocampal α7* and α9α10 nicotinic acetylcholine receptors by different mechanisms

2018 ◽  
Vol 100 ◽  
pp. 1-10 ◽  
Author(s):  
Hugo R. Arias ◽  
Elizabeth Vázquez-Gómez ◽  
Andy Hernández-Abrego ◽  
Sofía Gallino ◽  
Dominik Feuerbach ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Tricyclic Antidepressants ◽  
Nicotinic Acetylcholine

scholarly journals Post-processing of docking results through docking-based comparative intermolecular contacts analysis (dbCICA) of the α4β2 and α7 nicotinic acetylcholine receptors (nAChRs)

2020 ◽  
Author(s):  
Victor de Sousa Batista ◽  
Lourival Rodrigues de Sousa Neto ◽  
Roberto Ribeiro Faria ◽  
Keli Cristina Barbosa dos Reis ◽  
Nailton Monteiro do Nascimento Júnior
Keyword(s):  
Genetic Algorithm ◽  
Human Brain ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Ionic Channels ◽  
Post Processing ◽  
Nicotinic Acetylcholine ◽  
Neurologic Disorders ◽  
Α7 Nicotinic Acetylcholine Receptors ◽  
Intermolecular Contacts

The nAChRs are pentameric ligand-gated ionic channels that respond to the endogenous neurotransmitter acetylcholine, with the α4β2 and α7 subtypes being highly expressed in human brain. Those receptors are involved in many neurologic disorders such as Alzheimer’s disease and Schizophrenia, as well as in nicotine addiction. In this context, molecular modelling is a powerful tool for designing novel ligands targeting those receptors. In the present work, we applied dbCICA1 to identify optimal docking conditions for these two receptors. The methodology and results are summarized bellow. Briefly, bioactive compounds acting on each receptor where docked into the crystal structures obtained from PDB (5KXI2 for α4β2 and 5AFH3 for α7) using GOLD4 and the results were post-processed through dbCICA, a genetic algorithm based approach.

Molecular mechanisms of open-channel blockade in nicotinic acetylcholine receptors of autonomic ganglia neurons

1992 ◽  
Vol 70 (S1) ◽  
pp. S78-S85 ◽  
Author(s):  
Vladimir I. Skok
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Molecular Mechanisms ◽  
Open Channel ◽  
Ionic Channels ◽  
Channel Blockers ◽  
Autonomic Ganglia ◽  
Nicotinic Acetylcholine ◽  
Enteric Ganglia ◽  
Channel Blocking

The results of recent attempts to estimate the dimensions of ionic channels in nicotinic acetylcholine receptors of sympathetic and enteric ganglia neurons are reviewed. The channel dimensions, obtained from comparison of the sizes of the open-channel blocking molecules with their blocking activities, are 6.1 × 8.3 Å (1 Å = 0.1 nm) in both sympathetic and enteric ganglia. None of the competitive ganglionic blockers fit within this channel size. In addition, a chemical structure that binds the open-channel blockers in ganglionic nicotinic acetylcholine receptors is suggested to be formed by serine and threonine residues, as found by comparing the differences between the structures of the neuronal and muscle nicotinic acetylcholine receptors with the differences in their pharmacology.Key words: nicotinic acetylcholine receptor, autonomic ganglia, open-channel blocking mechanisms.

Nicotinic acetylcholine receptors in the patients with Parkinson's disease: 5IA-SPECT

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S586-S586 ◽  
Author(s):  
Kazuo Hashikawa ◽  
Hidefumi Yoshida ◽  
Nobukatsu Sawamoto ◽  
Shigetoshi Takaya ◽  
Chihiro Namiki ◽  
...  
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Nicotinic Acetylcholine
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