Inhibition by Anaesthetics of 14C-guanidinium Flux Through the Voltage-gated Sodium Channel and the Cation Channel of the 5-HT3 Receptor of N1E-115 Neuroblastoma Cells

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 1993 Feb 1

PMID 7682657

Citations 21

Authors

M Barann

M Gothert

K Fink

H Bonisch

Affiliations

Soon will be listed here.

Abstract

The influence of local and general anaesthetics on cation influx through the fast, voltage-dependent sodium channel and the 5-HT3 receptor cation channel was studied in N1E-115 mouse neuroblastoma cells by measuring 2-min influx of the organic cation 14C-guanidinium induced by either veratridine (1 mmol/l) or 5-HT (100 mumol/l). The veratridine-induced influx of 14C-guanidinium was potentiated by scorpion toxin and inhibited by tetrodotoxin. The 5-HT-induced 14C-guanidinium influx was not affected by tetrodotoxin but it was inhibited by nanomolar concentrations of the selective 5-HT3 receptor antagonists ondansetron and ICS 205-930; at high micromolar concentrations these compounds also inhibited the veratridine-induced influx of 14C-guanidinium. The 14C-guanidinium influx through both channels was inhibited by local and general anaesthetics. The rank order of potency for inhibition of veratridine-induced influx by local anaesthetics was tetracaine > bupivacaine > cocaine > lidocaine > procaine and that for inhibition of the 5-HT3 receptor channel was tetracaine > bupivacaine > cocaine > procaine > lidocaine. With the exception of procaine and cocaine, which were equipotent at both channels, the local anaesthetics were 4.4-fold (lidocaine) to 25-fold (tetracaine) more potent at the fast sodium channel than at the 5-HT3 receptor channel. The rank order of potency for general anaesthetics was propofol > etomidate = alfaxalone = ketamine > thiopental = methohexital at the fast sodium channel, and propofol > or = etomidate > alfaxalone = methohexital > thiopental > ketamine at the 5-HT3 receptor channel.(ABSTRACT TRUNCATED AT 250 WORDS)

Citing Articles

Serotonin and beyond-a tribute to Manfred Göthert (1939-2019).

Bonisch H, Fink K, Malinowska B, Molderings G, Schlicker E Naunyn Schmiedebergs Arch Pharmacol. 2021; 394(9):1829-1867.

PMID: 33991216 PMC: 8376721. DOI: 10.1007/s00210-021-02083-5.

Comparison of the effects of intravenous propofol and inhalational desflurane on the quality of early recovery after hand-assisted laparoscopic donor nephrectomy: a prospective, randomised controlled trial.

Park J, Kim M, Park Y, Shim J, Lee H, Kim Y BMJ Open. 2020; 10(12):e039881.

PMID: 33323432 PMC: 7745310. DOI: 10.1136/bmjopen-2020-039881.

Comparison of the impact of propofol versus sevoflurane on early postoperative recovery in living donors after laparoscopic donor nephrectomy: a prospective randomized controlled study.

Han S, Park J, Hong S, Lim S, Park Y, Chae M BMC Anesthesiol. 2020; 20(1):273.

PMID: 33115408 PMC: 7592560. DOI: 10.1186/s12871-020-01190-9.

Opportunities and Challenges for Single-Unit Recordings from Enteric Neurons in Awake Animals.

Barth B, Huang H, Hammer G, Shen X Micromachines (Basel). 2018; 9(9).

PMID: 30424361 PMC: 6187697. DOI: 10.3390/mi9090428.

Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids.

Herbrechter R, Ziemba P, Hoffmann K, Hatt H, Werner M, Gisselmann G Front Pharmacol. 2015; 6:130.

PMID: 26191003 PMC: 4490227. DOI: 10.3389/fphar.2015.00130.

References

Todd M, Drummond J, U H . The hemodynamic consequences of high-dose methohexital anesthesia in humans. Anesthesiology. 1984; 61(5):495-501. DOI: 10.1097/00000542-198411000-00003. View

Gothert M, Dorn W, Loewenstein I . Inhibition of catecholamine release from the adrenal medulla by halothane. Site and mechanism of action. Naunyn Schmiedebergs Arch Pharmacol. 1976; 294(3):239-49. DOI: 10.1007/BF00508391. View

Eckenhoff R, Shuman H . Saturable binding of halothane to rat brain synaptosomes. Proc Natl Acad Sci U S A. 1992; 89(10):4329-32. PMC: 49075. DOI: 10.1073/pnas.89.10.4329. View

Shafer A, Doze V, Shafer S, White P . Pharmacokinetics and pharmacodynamics of propofol infusions during general anesthesia. Anesthesiology. 1988; 69(3):348-56. DOI: 10.1097/00000542-198809000-00011. View

Benoit E, Carratu M, Dubois J, Mitolo-Chieppa D, Preziosi P . Electrophysiological studies of the effects of the general anaesthetic etomidate on frog myelinated nerve fibre. Br J Pharmacol. 1987; 90(1):7-14. PMC: 1917297. DOI: 10.1111/j.1476-5381.1987.tb16819.x. View

Burch P, Stanski D . The role of metabolism and protein binding in thiopental anesthesia. Anesthesiology. 1983; 58(2):146-52. DOI: 10.1097/00000542-198302000-00008. View

Olsen R . Drug interactions at the GABA receptor-ionophore complex. Annu Rev Pharmacol Toxicol. 1982; 22:245-77. DOI: 10.1146/annurev.pa.22.040182.001333. View

Tas P, Kress H, Koschel K . General anesthetics can competitively interfere with sensitive membrane proteins. Proc Natl Acad Sci U S A. 1987; 84(16):5972-5. PMC: 298985. DOI: 10.1073/pnas.84.16.5972. View

Neijt H, te Duits I, Vijverberg H . Pharmacological characterization of serotonin 5-HT3 receptor-mediated electrical response in cultured mouse neuroblastoma cells. Neuropharmacology. 1988; 27(3):301-7. DOI: 10.1016/0028-3908(88)90048-2. View

10.

Catterall W . Neurotoxins that act on voltage-sensitive sodium channels in excitable membranes. Annu Rev Pharmacol Toxicol. 1980; 20:15-43. DOI: 10.1146/annurev.pa.20.040180.000311. View

11.

Reiser G, Gunther A, Hamprecht B . Blockade by neurotransmitter antagonists of veratridine-activated ion channels in neuronal cell lines. J Neurochem. 1983; 40(2):493-502. DOI: 10.1111/j.1471-4159.1983.tb11310.x. View

12.

Hales T, Lambert J . The actions of propofol on inhibitory amino acid receptors of bovine adrenomedullary chromaffin cells and rodent central neurones. Br J Pharmacol. 1991; 104(3):619-28. PMC: 1908220. DOI: 10.1111/j.1476-5381.1991.tb12479.x. View

13.

Wieber J, Gugler R, Hengstmann J, DENGLER H . Pharmacokinetics of ketamine in man. Anaesthesist. 1975; 24(6):260-3. View

14.

Gothert M, Kennerknecht E, Thielecke G . Inhibition of receptor-mediated noradrenaline release from the sympathetic nerves of the isolated rabbit heart by anaesthetics and alcohols in proportion to their hydrophobic property. Naunyn Schmiedebergs Arch Pharmacol. 1976; 292(2):145-52. DOI: 10.1007/BF00498585. View

15.

Concas A, Santoro G, Mascia M, Serra M, Sanna E, Biggio G . The general anesthetic propofol enhances the function of gamma-aminobutyric acid-coupled chloride channel in the rat cerebral cortex. J Neurochem. 1990; 55(6):2135-8. DOI: 10.1111/j.1471-4159.1990.tb05807.x. View

16.

Cottrell G, Lambert J, Peters J . Modulation of GABAA receptor activity by alphaxalone. Br J Pharmacol. 1987; 90(3):491-500. PMC: 1917172. DOI: 10.1111/j.1476-5381.1987.tb11198.x. View

17.

Kilpatrick G, Bunce K, Tyers M . 5-HT3 receptors. Med Res Rev. 1990; 10(4):441-75. DOI: 10.1002/med.2610100404. View

18.

Kojda G, Klaus W, Werner G, Fricke U . The influence of 3-ester side chain variation on the cardiovascular profile of nitrendipine in porcine isolated trabeculae and coronary arteries. Naunyn Schmiedebergs Arch Pharmacol. 1991; 344(4):488-94. DOI: 10.1007/BF00172590. View

19.

Benoit E, Carratu M, Mitolo-Chieppa D . Interactions between molecules of a steroid anaesthetic (alphaxalone) and ionic channels of nodal membrane in voltage-clamped myelinated nerve fibre. Br J Pharmacol. 1988; 94(3):635-46. PMC: 1854051. DOI: 10.1111/j.1476-5381.1988.tb11570.x. View

20.

McNeal E, Lewandowski G, Daly J, Creveling C . [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985; 28(3):381-8. DOI: 10.1021/jm00381a019. View