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PMID: 5492893 Published · ppublish English Journal Article

Antagonism of 5-hydroxytryptamine by LSD 25 in the central nervous system: a possible neuronal basis for the actions of LSD 25.

British journal of pharmacology ·Vol. 40 ·No. 2 ·1970-10-00 ·Pages 202-18

Boakes RJ, Bradley PB, Briggs I, Dray A

Abstract

1. 5-Hydroxytryptamine (5-HT), acetylcholine (ACh), noradrenaline (NA), glutamate, D,L-homocysteic acid (DLH), glycine and gamma-aminobutyric acid (GABA) were applied to single neurones in the brain stem of decerebrate cats by microiontophoresis. The abilities of D-lysergic acid diethylamide tartrate (LSD 25), methysergide maleate (UML 491) and 2-bromo-lysergic acid diethylamide (BOL 148) to antagonize the actions of these compounds were studied.2. LSD 25 antagonized 5-HT excitation of single neurones when applied iontophoretically or administered intravenously. LSD 25 also antagonized glutamate excitation of neurones which could be excited by 5-HT. Inhibitory effects of 5-HT, the action of glutamate on neurones which could be inhibited by 5-HT and the actions of all the other compounds tested were unaffected by LSD 25.3. Iontophoretically applied UML 491 was also a specific antagonist to 5-HT and glutamate excitation but was less potent than LSD 25, and BOL 148 rarely exhibited antagonism.4. It is suggested that antagonism to 5-HT and glutamate excitation of brain stem neurones may be the basis of the psychotomimetic action of LSD 25. It is also suggested that there may be similarities in the mechanisms by which 5-HT and glutamate produce excitation where they act on the same neurone.

MeSH Terms
Acetylcholine/antagonists & inhibitors Aminobutyrates/antagonists & inhibitors Animals Brain Stem/drug effects Cats Drug Antagonism Female Glycine/antagonists & inhibitors Homocysteine/antagonists & inhibitors Iontophoresis Lysergic Acid Diethylamide/pharmacology Male Methysergide/pharmacology Neurons/drug effects Norepinephrine/antagonists & inhibitors Serotonin Antagonists Stimulation, Chemical
Chemicals
Aminobutyrates Serotonin Antagonists Homocysteine Lysergic Acid Diethylamide Acetylcholine Glycine Norepinephrine Methysergide
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Boakes R J
Bradley P B
Briggs I
Dray A
References (48)
48 references, click to expand
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Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
DOI
10.1111/j.1476-5381.1970.tb09914.x
Published
1970-10-00
Pages
202-18
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1702892
Subset
IM
External Links
PubMed source DOI: 10.1111/j.1476-5381.1970.tb09914.x PMC Full Text View journal details
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