On the mechanism of action of the antidepressant drugs amitriptyline and nortriptyline. Evidence for 5-hydroxytryptamine receptor blocking activity

Kjell Fuxe; Sven ove Ögren; Luigi Agnati; Jan Åke Gustafsson; Gösta Jonsson

doi:10.1016/0304-3940(77)90095-7

On the mechanism of action of the antidepressant drugs amitriptyline and nortriptyline. Evidence for 5-hydroxytryptamine receptor blocking activity

Kjell Fuxe, Sven ove Ögren, Luigi Agnati, Jan Åke Gustafsson, Gösta Jonsson

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

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Abstract

Effects of amitryptyline (AMI) and nortriptyline (NOR) were studied on the [5-³H] hydroxytryptamine ([5-³H]HT) and D-[³H]lysergic acid diethylamide-(D-[³H] LSD) binding in cerebral cortex of rats and on behaviours depedent upon 5-hydroxtrryptamine (5-HT) receptor activity. AMI and NOR were found to have affinity for some of the D-LSD binding sites in the cerebral cortex but no or very weak affinity for the 5-HT binding site. AMI and NOR blocked the 5-hydroxytryptophan (5-HTP) and D-LSD induced head twitches in mice and the D-LSD induced extensor reflex activity. This 5-HT receptor blocking activity of AMI and NOR may in part mediate their antidepressant actions.

Original language	English (US)
Pages (from-to)	339-343
Number of pages	5
Journal	Neuroscience Letters
Volume	6
Issue number	4
DOIs	https://doi.org/10.1016/0304-3940(77)90095-7
State	Published - Dec 1977

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Neuroscience(all)

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10.1016/0304-3940(77)90095-7

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title = "On the mechanism of action of the antidepressant drugs amitriptyline and nortriptyline. Evidence for 5-hydroxytryptamine receptor blocking activity",

abstract = "Effects of amitryptyline (AMI) and nortriptyline (NOR) were studied on the [5-3H] hydroxytryptamine ([5-3H]HT) and D-[3H]lysergic acid diethylamide-(D-[3H] LSD) binding in cerebral cortex of rats and on behaviours depedent upon 5-hydroxtrryptamine (5-HT) receptor activity. AMI and NOR were found to have affinity for some of the D-LSD binding sites in the cerebral cortex but no or very weak affinity for the 5-HT binding site. AMI and NOR blocked the 5-hydroxytryptophan (5-HTP) and D-LSD induced head twitches in mice and the D-LSD induced extensor reflex activity. This 5-HT receptor blocking activity of AMI and NOR may in part mediate their antidepressant actions.",

author = "Kjell Fuxe and {\"O}gren, {Sven ove} and Luigi Agnati and Gustafsson, {Jan {\AA}ke} and G{\"o}sta Jonsson",

note = "Funding Information: This work has been supported by a grant (04X-715) from the Swedish Medical Research Council and by a grant (MH 25504-04) from the National Institute of Health. The skilful technical assistance of Mrs. A.-C. Holm, ~rs. U.-B. Finnman and Miss B. H~an is gratefully acknowledged. Copyright: Copyright 2014 Elsevier B.V., All rights reserved.",

year = "1977",

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doi = "10.1016/0304-3940(77)90095-7",

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AU - Ögren, Sven ove

AU - Agnati, Luigi

AU - Gustafsson, Jan Åke

AU - Jonsson, Gösta

N1 - Funding Information: This work has been supported by a grant (04X-715) from the Swedish Medical Research Council and by a grant (MH 25504-04) from the National Institute of Health. The skilful technical assistance of Mrs. A.-C. Holm, ~rs. U.-B. Finnman and Miss B. H~an is gratefully acknowledged. Copyright: Copyright 2014 Elsevier B.V., All rights reserved.

PY - 1977/12

Y1 - 1977/12

N2 - Effects of amitryptyline (AMI) and nortriptyline (NOR) were studied on the [5-3H] hydroxytryptamine ([5-3H]HT) and D-[3H]lysergic acid diethylamide-(D-[3H] LSD) binding in cerebral cortex of rats and on behaviours depedent upon 5-hydroxtrryptamine (5-HT) receptor activity. AMI and NOR were found to have affinity for some of the D-LSD binding sites in the cerebral cortex but no or very weak affinity for the 5-HT binding site. AMI and NOR blocked the 5-hydroxytryptophan (5-HTP) and D-LSD induced head twitches in mice and the D-LSD induced extensor reflex activity. This 5-HT receptor blocking activity of AMI and NOR may in part mediate their antidepressant actions.

AB - Effects of amitryptyline (AMI) and nortriptyline (NOR) were studied on the [5-3H] hydroxytryptamine ([5-3H]HT) and D-[3H]lysergic acid diethylamide-(D-[3H] LSD) binding in cerebral cortex of rats and on behaviours depedent upon 5-hydroxtrryptamine (5-HT) receptor activity. AMI and NOR were found to have affinity for some of the D-LSD binding sites in the cerebral cortex but no or very weak affinity for the 5-HT binding site. AMI and NOR blocked the 5-hydroxytryptophan (5-HTP) and D-LSD induced head twitches in mice and the D-LSD induced extensor reflex activity. This 5-HT receptor blocking activity of AMI and NOR may in part mediate their antidepressant actions.

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On the mechanism of action of the antidepressant drugs amitriptyline and nortriptyline. Evidence for 5-hydroxytryptamine receptor blocking activity

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