The Analgesic and Anaesthetic Actions of Tetrafluorobenzene

Neal, M. J.; Robson, J. M.

doi:10.1111/j.1476-5381.1966.tb01929.x

Cited by 4 publications

(2 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Although not used as clinical anesthetics, volatile aromatic compounds have industrial applications, are drugs of abuse, and have anesthetic effects 15. They inhibit NMDA receptor function,16 and potentiate GABA A receptor function,17 doing so in a reciprocal manner: the aromatic anesthetics which inhibit NMDA receptors best enhance GABA A receptor function the least.…”

Section: Introductionmentioning

confidence: 99%

The Effects of Volatile Aromatic Anesthetics on Voltage-Gated Na+ Channels Expressed in Xenopus Oocytes

Horishita

Eger

Harris³

2008

Anesthesia &Amp; Analgesia

View full text Add to dashboard Cite

Background-Many inhaled anesthetics inhibit voltage-gated sodium channels at clinically relevant concentrations, and suppression of neurotransmitter release by these agents results, at least partly, from decreased presynaptic sodium channel activity. Volatile aromatic anesthetics can inhibit N-methyl-D-aspartate (NMDA) receptor function and enhance γ-amino butyric acid A (GABA A ) receptor function, but these effects depend strongly on the chemical properties of the aromatic ompounds. The present study tested whether diverse aromatic anesthetics consistently inhibit sodium channel function.

show abstract

Section: Introductionmentioning

confidence: 99%

The Effects of Volatile Aromatic Anesthetics on Voltage-Gated Na+ Channels Expressed in Xenopus Oocytes

Horishita

Eger

Harris³

2008

Anesthesia &Amp; Analgesia

View full text Add to dashboard Cite

show abstract

“…Some may also be inhaled to produce dizziness, learning and memory impairment, and even unconsciousness, and thus they are general anesthetics (Neal and Robson, 1966;Massey and Jackson, 1973;Fang et al, 1996;Balster, 1998). By virtue of their electrons, these inhalants may engage in electrostatic interactions with protein residues that possess cationic atomic charge (Mecozzi et al, 1996).…”

mentioning

confidence: 99%

The N-Methyl-d-aspartate Receptor Inhibitory Potencies of Aromatic Inhaled Drugs of Abuse: Evidence for Modulation by Cation-π Interactions

Raines

Gioia²,

Claycomb³

et al. 2004

J Pharmacol Exp Ther

View full text Add to dashboard Cite

Benzene and several close structural analogs are inhaled drugs of abuse with general anesthetic activity. By virtue of their electron clouds, they may engage in attractive electrostatic interactions with cationic atomic charges on protein targets. In this study, we tested the hypothesis that inhaled drugs of abuse inhibit human N-methyl-D-aspartate (NMDA) receptors with potencies that correlate with their abilities to engage in cationinteractions. Electrophysiological techniques were used to define the NR1/NR2B NMDA receptor inhibitory concentrations of volatile benzene analogs, and computer modeling was used to quantify their abilities to engage in cation-interactions and their molecular volumes. In addition, each compound's octanol/ gas partition coefficient (a measure of hydrophobicity) was quantified. All 18 compounds inhibited human NR1/NR2B NMDA receptors reversibly and in a concentration-dependent manner. NMDA receptor inhibitory potency correlated strongly with the ability to engage in cation-interactions, weakly with hydrophobicity, and was independent of molecular volume. This is consistent with the hypothesis that cation-interactions enhance the binding of inhaled drugs of abuse to the NMDA receptor and suggests that the receptor binding site(s) for these drugs possesses significant cationic character.

show abstract

Wt19f

Francl

2023

Nat. Chem.

View full text Add to dashboard Cite

The Analgesic and Anaesthetic Actions of Tetrafluorobenzene

Cited by 4 publications

References 15 publications

The Effects of Volatile Aromatic Anesthetics on Voltage-Gated Na+ Channels Expressed in Xenopus Oocytes

The Effects of Volatile Aromatic Anesthetics on Voltage-Gated Na+ Channels Expressed in Xenopus Oocytes

The N-Methyl-d-aspartate Receptor Inhibitory Potencies of Aromatic Inhaled Drugs of Abuse: Evidence for Modulation by Cation-π Interactions

Wt19f

Contact Info

Product

Resources

About