Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter

Dan C. Martin; Robert P. Introna; Robert S. Aronstam

doi:10.1016/0304-3940(90)90329-8

Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter

Dan C. Martin
, Robert P. Introna
, Robert S. Aronstam

Anesthesiology and Perioperative Medicine

Research output: Contribution to journal › Article › peer-review

43 Scopus citations

Abstract

The effects of halothane and ketamine on (1) serotonin (5-hydroxytryptamine; 5-HT) uptake and (2) paroxetine binding to the 5-HT transporter in neuronal membranes were determined in rat brain. Both anesthetics inhibited the uptake of [³H]5-HT by synaptosomes, but only ketamine affected binding of [³H]paroxetine to the 5-HT transporter. Saturation analysis indicated that ketamine inhibition of [³H]paroxetine binding was competitive (K_i = 18.8 μM). These results indicate that halothane and ketamine inhibit 5-HT transport by different mechanisms.

Original language	English (US)
Pages (from-to)	99-103
Number of pages	5
Journal	Neuroscience Letters
Volume	112
Issue number	1
DOIs	https://doi.org/10.1016/0304-3940(90)90329-8
State	Published - Apr 20 1990

Keywords

5-Hydroxytryptamine
Anesthetic
Brain
Halothane
Imipramine
Ketamine
Paroxetine
Serotonin
Serotonin receptor
Serotonin uptake

ASJC Scopus subject areas

General Neuroscience

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10.1016/0304-3940(90)90329-8

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title = "Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter",

abstract = "The effects of halothane and ketamine on (1) serotonin (5-hydroxytryptamine; 5-HT) uptake and (2) paroxetine binding to the 5-HT transporter in neuronal membranes were determined in rat brain. Both anesthetics inhibited the uptake of [3H]5-HT by synaptosomes, but only ketamine affected binding of [3H]paroxetine to the 5-HT transporter. Saturation analysis indicated that ketamine inhibition of [3H]paroxetine binding was competitive (Ki = 18.8 μM). These results indicate that halothane and ketamine inhibit 5-HT transport by different mechanisms.",

keywords = "5-Hydroxytryptamine, Anesthetic, Brain, Halothane, Imipramine, Ketamine, Paroxetine, Serotonin, Serotonin receptor, Serotonin uptake",

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doi = "10.1016/0304-3940(90)90329-8",

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T1 - Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter

AU - Martin, Dan C.

AU - Introna, Robert P.

AU - Aronstam, Robert S.

PY - 1990/4/20

Y1 - 1990/4/20

N2 - The effects of halothane and ketamine on (1) serotonin (5-hydroxytryptamine; 5-HT) uptake and (2) paroxetine binding to the 5-HT transporter in neuronal membranes were determined in rat brain. Both anesthetics inhibited the uptake of [3H]5-HT by synaptosomes, but only ketamine affected binding of [3H]paroxetine to the 5-HT transporter. Saturation analysis indicated that ketamine inhibition of [3H]paroxetine binding was competitive (Ki = 18.8 μM). These results indicate that halothane and ketamine inhibit 5-HT transport by different mechanisms.

AB - The effects of halothane and ketamine on (1) serotonin (5-hydroxytryptamine; 5-HT) uptake and (2) paroxetine binding to the 5-HT transporter in neuronal membranes were determined in rat brain. Both anesthetics inhibited the uptake of [3H]5-HT by synaptosomes, but only ketamine affected binding of [3H]paroxetine to the 5-HT transporter. Saturation analysis indicated that ketamine inhibition of [3H]paroxetine binding was competitive (Ki = 18.8 μM). These results indicate that halothane and ketamine inhibit 5-HT transport by different mechanisms.

KW - 5-Hydroxytryptamine

KW - Anesthetic

KW - Brain

KW - Halothane

KW - Imipramine

KW - Ketamine

KW - Paroxetine

KW - Serotonin

KW - Serotonin receptor

KW - Serotonin uptake

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U2 - 10.1016/0304-3940(90)90329-8

DO - 10.1016/0304-3940(90)90329-8

M3 - Article

C2 - 2143567

AN - SCOPUS:0025318248

SN - 0304-3940

VL - 112

SP - 99

EP - 103

JO - Neuroscience Letters

JF - Neuroscience Letters

IS - 1

ER -

Inhibition of neuronal 5-HT uptake by ketamine, but not halothane, involves disruption of substrate recognition by the transporter

Abstract

Keywords

ASJC Scopus subject areas

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