The sodium channels of the neuroblastoma x glioma 108 CC 15 hybrid cell change their sensitivity for volatile and local anesthetics upon continuous passage

1989 ◽  
Vol 76 (2) ◽  
pp. 99-107 ◽  
Author(s):  
P. W. L. Tas ◽  
H. G. Kress ◽  
K. Koschel
Keyword(s):  
Sodium Channels ◽  
Local Anesthetics ◽  
Hybrid Cell

scholarly journals Atomic determinants of state-dependent block of sodium channels by charged local anesthetics and benzocaine

FEBS Letters ◽  
2006 ◽  
Vol 580 (26) ◽  
pp. 6027-6032 ◽  
Author(s):  
Denis B. Tikhonov ◽  
Iva Bruhova ◽  
Boris S. Zhorov
Keyword(s):  
Sodium Channels ◽  
Local Anesthetics ◽  
State Dependent

Spectral Investigations, Molecular Interactions and Electrochemical Studies of (2R)-(-)2-(2, 6-dimethylphenylaminocarbonyl)-1-methyl Piperidinium Chloride

2020 ◽  
Vol 15 (4) ◽  
pp. 358-368
Author(s):  
J. Deva Anban ◽  
J. Sharmi Kumar ◽  
C. James ◽  
Sayantan Pradhan
Keyword(s):  
Sodium Channels ◽  
Local Anesthetics ◽  
Natural Bond Orbital ◽  
Nbo Analysis ◽  
Basis Set ◽  
Voltage Gated ◽  
Peripheral Neurons ◽  
Voltage Gated Sodium Channels ◽  
Title Molecule ◽  
Inner Pore

Background: Local anesthetics are widely used to decrease sensitivity to pain in specific regions of the body while performing medical tasks. Many studies have probed the mechanism of action of local anesthetics but still many questions remain. (2R - (-) 2 - (2, 6-dimethylphenylaminocarbonyl) - 1 – methyl piperidinium chloride (DAMP), is an extensively used amide-type local anesthetic. Objective: This study aims at revealing the various electrophysical and chemical properties of the title compound. This study will be useful for future research by pharmacologists. Method: Density Functional Theory (DFT) computations were executed using Gaussian’09 program package and were optimized with the B3LYP /6-311+G (d, p) basis set. Natural bond orbital (NBO) analysis was carried out with version 3.1. Normal Coordinate Analysis (NCA) was used to systematically calculate the harmonic vibrational wavenumbers. Molecular docking simulations were carried out to understand the pharmacokinetic behavior of the drug. Results: The presence of strong N-H…Cl intra molecular hydrogen bonding was evidently revealed from the FT-IR spectrum due to the shifting of NH stretching wavenumber. Stability of the molecule arising from hyper conjugative interactions exhibits the bioactivity of the molecule by natural bond orbital analysis. The title molecule binds to the inner pore and blocks voltage - gated sodium channels in peripheral neurons. Conclusion: A detailed molecular picture of DAMP and its interactions were obtained by modeling analysis, IR, Raman, and UV-Vis spectroscopy. The geometrical parameters agree well with the XRD data. NBO analysis indicates the bioactivity of the molecule. The HOMO-LUMO energy gap indicates the possibility of intramolecular charge transfer of the molecule. From the ligand docking studies it is concluded that the title molecule binds to the inner pore and blocks voltage - gated sodium channels in peripheral neurons.

LOCAL ANESTHETICS MANIFEST TWO DISTINCT MODES OF BLOCKADE OF SINGLE SODIUM CHANNELS

1991 ◽  
Vol 75 (3) ◽  
pp. A687-A687
Author(s):  
K. Gingrich ◽  
D. Beardsley ◽  
D. Yue
Keyword(s):  
Sodium Channels ◽  
Local Anesthetics ◽  
Single Sodium Channels

Retarded recovery of excitability and twitches of frog toe muscles after K-induced depolarization (slow inactivation) in the presence of alkyl amphipaths

1985 ◽  
Vol 63 (10) ◽  
pp. 1335-1338
Author(s):  
James G. Foulks ◽  
Lillian Morishita
Keyword(s):  
Low Temperature ◽  
Sodium Channels ◽  
Local Anesthetics ◽  
Slow Inactivation ◽  
Frequency Dependent ◽  
High K

Alkyl amphipaths resemble conventional local anesthetics in their ability to retard the recovery of excitability and twitch tension after depolarization at high Ko, an effect that is attributed to slow inactivation of potential-dependent sodium channels. The similar effect of low temperature offers an explanation for its ability to enhance the frequency-dependent effects of these agents.

The influence of temperature and frequency of stimulation on the impairment of excitability of frog skeletal muscle by local anesthetics and alkyl amphipathic agents

1985 ◽  
Vol 63 (10) ◽  
pp. 1327-1334 ◽  
Author(s):  
James G. Foulks ◽  
Lillian Morishita
Keyword(s):  
Skeletal Muscle ◽  
Sodium Channels ◽  
Local Anesthetics ◽  
Frog Skeletal Muscle ◽  
Abrupt Increase ◽  
Frequency Dependent ◽  
Temperature Changes ◽  
Influence Of Temperature ◽  
Lipid Environment ◽  
Frequency Of Stimulation

The potency of various types of alkyl amphipathic (cationic, anionic, and neutral) as well as tertiary amine local anesthetics in impairing the excitability of frog skeletal muscle was markedly enhanced by an increase in temperature from 20 to 30 °C. Enhancement of the local anesthetic effects of all types of agents was also produced by a decrease in temperature to 5 °C, but this effect was found to be frequency dependent. With abrupt increase or decrease in temperature, changes in excitability were rapid and unlikely to be the result of changes in the partition of the apolar portions of these molecules into the hydrophobic regions of the sarcolemma. These results are interpreted as indicating that both the presence of local anesthetics and alterations in temperature can influence the rates of potential-dependent changes in the conformation of membrane proteins that control the permeability of excitable sodium channels, possibly by modifying the fluidity of specific portions of their hydrophobic components or their immediate lipid environment. The accumulation of inactivation as the result of incomplete recovery from the effects of preceding depolarizations appears sufficient to explain the frequency-dependent effects produced by these agents.

Molecular determinants of prokaryotic voltage-gated sodium channels for recognition of local anesthetics

FEBS Journal ◽  
2016 ◽  
Vol 283 (15) ◽  
pp. 2881-2895 ◽  
Author(s):  
Takushi Shimomura ◽  
Katsumasa Irie ◽  
Yoshinori Fujiyoshi
Keyword(s):  
Sodium Channels ◽  
Local Anesthetics ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels ◽  
Molecular Determinants
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