Citalopram antagonizes the stimulation by lysergic acid diethylamide of presynaptic inhibitory serotonin autoreceptors in the rat hypothalamus.

Slices of rat hypothalamus prelabeled with [3H]-5-hydroxytryptamine ([3H]-5-HT) were superfused and the release of the labeled transmitter was elicited either by electrical stimulation or by fenfluramine. Whereas the electrically stimulated release of [3H]-5-HT was completely abolished by removing calcium from the superfusion medium, the fenfluramine-induced release of [3H]-5-HT was calcium-independent. Methiothepin increased, in a concentration-dependent manner, the [3H]-5-HT release induced by electrical stimulation but had no effect on that elicited by fenfluramine. The 3H-transmitter release elicited by electrical stimulation was inhibited by lysergic acid diethylamide (LSD) in a concentration-dependent manner, but the release induced by fenfluramine was not modified by LSD. The reduction by LSD of [3H]-5-HT overflow elicited by electrical stimulation was antagonized by methiothepin, but unaffected by phentolamine or by sulpiride. Low concentrations (10-1000 nM) of citalopram, a 5-HT uptake inhibitor, antagonized the inhibition by LSD of electrically evoked release of [3H]-5-HT. These concentrations of citalopram did not modify by themselves the overflow of [3H]-5-HT elicited by electrical stimulation. It is concluded that the modulation of [3H]-5-HT release by presynaptic serotonin autoreceptors is not operational when the neurotransmitter is released through a calcium-independent mechanism. The potent presynaptic inhibition by LSD of serotonergic neurotransmission may contribute to the central actions of this drug. The interaction between citalopram and LSD at the level of [3H]-5-HT release does not seem to involve a competitive interaction at the same receptor site. The possibility that neuronal uptake of 5-HT and the presynaptic 5-HT autoreceptor may be linked in a functional manner cannot be excluded.

• Publication year

  1982

• Venue

  Journal of Pharmacology and Experimental Therapeutics

• Publication date

  1982-07-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/s0022-3565(25)33177-0PMID 6953233
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• The effects of d-amphetamine and potassium on serotonin release and metabolism in rat cerebral cortex tissue.

  1981cited by this paper
• Stereoselectivity of presynaptic autoreceptors modulating dopamine release.

  1981cited by this paper
• Further evidence for negative feedback control of serotonin release in the central nervous system

  1981cited by this paper
• Presynaptic modulation of the release of dopamine from the rabbit caudate nucleus: differences between electrical stimulation, amphetamine and tyramine.

  1981cited by this paper
• Noradrenaline inhibits depolarization-induced 3H-serotonin release from slices of rat hippocampus.

  1980cited by this paper
• High-affinity [3H]imipramine binding in rat hypothalamus: association with uptake of serotonin but not of norepinephrine.

  1980cited by this paper
• Inhibition of neuronal uptake reduces the presynaptic effects of clonidine but not of alpha-methylnoradrenaline on the stimulation-evoked release of 3H-noradrenaline from rat occipital cortex slices.

  1980cited by this paper
• Alpha-adrenoceptor-mediated modulation of 5-hydroxytryptamine release from rat brain cortex slices

  1980cited by this paper
• Serotonin-receptor-mediated modulation of Ca2+-dependent 5-hydroxytryptamine release from neurones of the rat brain cortex

  1980cited by this paper
• EVIDENCE FOR TWO TYPES OF EXCITATORY RECEPTOR FOR 5‐HYDROXYTRYPTAMINE IN DOG ISOLATED VASCULATURE

  1980cited by this paper
• Presynaptic regulation of the release of catecholamines.

  1980cited by this paper
• Extracellular 5-hydroxytryptamine inhibits 5-hydroxytryptamine release from rat brain cortex slices

  1979cited by this paper
• Multiple serotonin receptors: differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol.

  1979cited by this paper
• Facilitation by GABA of the potassium-evoked release of 3H-noradrenaline from the rat occipital cortex

  1979cited by this paper
• Serotonin release is modulated by presynaptic autoreceptors.

  1979cited by this paper
• Acute changes in central serotonin metabolism induced by the blockade or stimulation of serotoninergic receptors during ontogenesis in the rat.

  1977cited by this paper
• SIXTH GADDUM MEMORIAL LECTURE NATIONAL INSTITUTE FOR MEDICAL RESEARCH, MILL HILL, JANUARY 1977

  1977cited by this paper
• Calcium-dependent release of endogenous serotonin, dopamine and norepinephrine from nerve endings.

  1977cited by this paper
• Regulation of noradrenaline release by presynaptic receptor systems.

  1977cited by this paper
• The action of fenfluramine andp-chloramphetamine on serotonergic mechanisms: A comparative study in rat brain nuclei

  1976cited by this paper
• Calcium-dependent release of radiolabeled catecholamines and serotonin from rat brain synaptosomes in a superfusion system.

  1975cited by this paper
• Effect of thioridazine, clozapine and other antipsychotics on the kinetic state of tyrosine hydroxylase and on the turnover rate of dopamine in striatum and nucleus accumbens.

  1975cited by this paper
• Lysergic acid diethylamide: evidence for stimulation of cerebral dopamine receptors.

  1975cited by this paper
• THE EFFECTS OF LYSERGIC ACID DIETHYLAMIDE ON THE RESPONSE TO FIELD STIMULATION OF THE RAT VAS DEFERENS AND THE RAT AND CAT ANOCOCCYGEUS MUSCLES

  1975cited by this paper
• Presynaptic regulation of catecholamine release.

  1974cited by this paper
• LSD as an agonist and antagonist at central dopamine receptors

  1974cited by this paper
• Effects of LSD on synthesis and release of 5-HT in rat brain slices.

  1974cited by this paper
• Influence of drugs with affinity for alpha-adrenoceptors on noradrenaline release by potassium, tyramine and dimethylphenylpiperazinium.

  1974cited by this paper
• Drug-induced changes in the release of 3 H-monoamines from field stimulated rat brain slices.

  1971cited by this paper
• RELEASE OF [3H]SEROTONIN FROM BRAIN SLICES 1

  1969cited by this paper
• [Increase of noradrenaline effects by tyramine].

  1965cited by this paper

• The effects of electroconvulsive therapy and antidepressant drugs on monoamine receptors in rodent brain--similarities and differences.

  2007cites this paper
• The pharmacology of the neurochemical transmission in the midbrain raphe nuclei of the rat.

  2006cites this paper
• In vivo effects of local activation and blockade of 5-HT1B receptors on globus pallidus neuronal spiking.

  2005cites this paper
• Frequency-dependence of serotonin autoreceptor but not α2-adrenoceptor inhibition of [3H]-serotonin release in rat hypothalamic slices

  2004cites this paper
• Neuropharmacological reassessment of the discriminative stimulus properties ofd-lysergic acid diethylamide (LSD)

  2004cites this paper
• Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites

  2004cites this paper
• Functional Neuropharmacology of Compounds Acting at 5-HT1B/D Receptors

  2000cites this paper
• Autoregulation of serotonin neurons: role in antidepressant drug action.

  1999cites this paper
• Cannabinoid transmission and reward-related events.

  1998cites this paper
• Serotonin Transporter Function in vivo: Assessment by Chronoamperometry a

  1998cites this paper
• 5-HT autoreceptors in the regulation of 5-HT release from guinea pig raphe nucleus and hypothalamus.

  1997cites this paper
• Quantitative microdialysis of serotonin and norepinephrine: pharmacological influences on in vivo extraction fraction.

  1996cites this paper
• Isolation and Characterization of an Endogenous Peptide from Rat Brain Interacting Specifically with the Serotonergic 1B Receptor Subtypes (*)

  1996cites this paper
• Complex stimulus properties of LSD: a drug discrimination study with α2-adrenoceptor agonists and antagonists

  1995cites this paper
• Effect of milnacipran and desipramine on noradrenergic alpha 2-autoreceptor sensitivity.

  1994cites this paper
• Effects of LSD on Ca++ currents in central 5-HT-containing neurons: 5-HT1A receptors may play a role in hallucinogenesis.

  1994cites this paper
• Neuropharmacology of 5-hydroxytryptamine1B/D receptor ligands.

  1994cites this paper
• Fenfluramine Releases Serotonin from Human Brain Nerve Endings by a Dual Mechanism

  1994cites this paper
• Relevance of 5-HT autoreceptors for psychotropic drug action.

  1993cites this paper
• Antagonism by citalopram and tianeptine of presynaptic 5-HT1B heteroreceptors inhibiting acetylcholine release.

  1993cites this paper
• The unique effect of methiothepin on the terminal serotonin autoreceptor in the rat hypothalamus could be an example of inverse agonism

  1993cites this paper
• Effect of lithium on the prolactin response to D-fenfluramine in healthy subjects.

  1993cites this paper
• Functional characterization of a 5‐HT3 receptor which modulates the release of 5‐HT in the guinea‐pig brain

  1993cites this paper
• Neurobiological mechanisms involved in antidepressant therapies.

  1993cites this paper
• Evidence of an exocytotic-like release of [3H]5-hydroxytryptamine induced by d-fenfluramine in rat hippocampal synaptosomes.

  1993cites this paper
• Effects of methiothepin on changes in brain serotonin release induced by repeated administration of high doses of anorectic serotoninergic drugs.

  1992cites this paper
• Fluoxetine-induced inhibition of synaptosomal [3H]5-HT release: possible Ca(2+)-channel inhibition.

  1992cites this paper
• Characterization of the 5‐Hydroxytryptamine Receptor Modulating the Release of 5‐[3H]Hydroxytryptamine in Slices of the Human Neocortex

  1992cites this paper
• Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release.

  1992cites this paper
• Evidence Against a Direct Link Between Serotonin Uptake Sites and Presynaptic Serotonin Autoreceptors

  1991cites this paper
• Terminal serotonin autoreceptor function in the rat hippocampus is not modified by pertussis and cholera toxins

  1991cites this paper
• Antagonism by antidepressant drugs of the inhibitory effect of trifluoromethylphenylpiperazine (TFMPP) on [3H]acetylcholine release in rat or guinea-pig hippocampal synaptosomes.

  1991cites this paper
• Presynaptic and postsynaptic modifications of the serotonin system by long-term administration of antidepressant treatments. An in vivo electrophysiologic study in the rat.

  1991cites this paper
• The Inhibitory Effect of Trifluoromethylphenylpiperazine on [3H]Acetylcholine Release in Guinea Pig Hippocampal Synaptosomes Is Mediated by a 5‐Hydroxytryptamine1 Receptor Distinct from 1A, 1B, and 1C Subtypes

  1991cites this paper
• Marijuana's interaction with brain reward systems: update 1991.

  1991cites this paper
• Serotonin regulation of tachykinin biosynthesis in the rat neostriatum.

  1991cites this paper
• The 5-HT transporter is an additional site of action for the 5-HT agonists RU 24969 and TFMPP

  1991cites this paper
• Different Interactions of Citalopram with the Prejunctional Effects of Serotonin in Peripheral Tissues

  1991cites this paper
• TFMPP and RU24969 enhance serotonin release from rat hippocampus.

  1990cites this paper
• Release by U-50,488H of [3H]serotonin from brain slices and spinal cord synaptosomes of U-50,488H-tolerant and nontolerant mice.

  1990cites this paper
• Interaction between serotonin uptake inhibitors and alpha-2 adrenergic heteroreceptors in the rat hypothalamus.

  1990cites this paper
• MDMA (ecstasy) effects on cultured serotonergic neurons: evidence for Ca2(+)-dependent toxicity linked to release.

  1990cites this paper
• Serotonin

  1990cites this paper
• Serotonin uptake blockers influence serotonin autoreceptors by increasing the biophase concentration of serotonin and not through a “molecular link”

  1990cites this paper
• Electrophysiological Investigation of the Effects of Antidepressant Treatments on Serotonin Receptors

  1990cites this paper
• Autoreceptor control of 5-HT release from central serotoninergic neurones.

  1990cites this paper
• Modulation of [3H]serotonin release by dihydropyridines in spinal cord synaptosomes.

  1990cites this paper
• Dopamine uptake: a review of progress in the last decade.

  1990cites this paper
• TFMPP and RU24969 enhance serotonin release rat hipocampus

  1990cites this paper
• Modulation by drugs of the release of total tritium and 3H-5-HT from rat hypothalamic slices

  1990cites this paper
• Behavioral mechanisms for the anorectic action of the serotonin (5-HT) uptake inhibitor sertraline in rats: comparison with directly acting 5-HT agonists.

  1990cites this paper
• Serotonin receptor activation reduces calcium current in an acutely dissociated adult central neuron.

  1990cites this paper
• Autorécepteur sérotoninergique et antidépresseurs

  1990cites this paper
• Presynaptic Serotonin Receptors in the Central Nervous System

  1990cites this paper
• Modulation of neurotransmitter release by presynaptic autoreceptors.

  1989cites this paper
• Different Recognition Sites for Serotonin: The Neuronal Na+-dependent Transporter and the Release-modulating Autoreceptor

  1989cites this paper
• Diurnal Variation in the Function of Serotonin Terminals in the Rat Hypothalamus

  1989cites this paper
• Phorbol‐12,13‐dibutyrate antagonizes while forskolin potentiates the presynaptic autoreceptor‐mediated inhibition of [3H]‐5‐hydroxytryptamine release in rat hypothalamic slices

  1989cites this paper
• Involvement of adenylate cyclase and protein kinase C in the α2-adrenoceptor-mediated inhibition of noradrenaline and 5-hydroxytryptamine release in rat hypothalamic slices

  1989cites this paper
• Serotonin

  1989cites this paper
• Amphetamine antagonizes the presynaptic inhibitory effect of clonidine through an interaction at the level of the alpha 2-adrenoceptors.

  1989cites this paper
• 5-HT Receptors Mediating Pre-synaptic Autoinhibition in Central Serotoninergic Nerve Terminals

  1989cites this paper
• Effect of Chronic Lithium Treatment on 5‐Hydroxytryptamine Autoreceptors and Release of 5‐[3H]Hydroxytryptamine from Rat Brain Cortical, Hippocampal, and Hypothalamic Slices

  1988cites this paper
• Autoreceptors Regulating Serotonin Release

  1988cites this paper
• Long-term 5-HT reuptake blockade, but not monoamine oxidase inhibition, decreases the function of terminal 5-HT autoreceptors: an electrophysiological study in the rat brain

  1988cites this paper
• Presynaptic Receptors on Catecholamine Neurones

  1988cites this paper
• Modulation of 5-HT Autoreceptors Probably Contributes to the Antidepressant Action of 5-HT Uptake Blockers

  1988cites this paper
• Modulation of Transmitter Release by Presynaptic Serotonin Receptors

  1988cites this paper
• Sensitivity of the response of 5-HT autoreceptors to drugs modifying synaptic availability of 5-HT.

  1988cites this paper
• Modulation of the Electrically Evoked Release of 5‐[3H]Hydroxytryptamine from Rat Cerebral Cortex: Effects of Alpidem, CL 218872, and Diazepam

  1988cites this paper
• Tryptophan hydroxylase activity in brain slices.

  1988cites this paper
• Proceedings of the British Pharmacological Society. 6th-8th January, 1988. Abstracts.

  1988cites this paper
• Presynaptic serotonin receptors and alpha-adrenoceptors on central serotoninergic and noradrenergic neurons of normotensive and spontaneously hypertensive rats.

  1988cites this paper
• A functional response to D1 dopamine receptor stimulation in the central nervous system: inhibition of the release of [3H]-serotonin from the rat substantia nigra

  1987cites this paper
• Interaction between 5-HT uptake inhibition and activation of 5-HT autoreceptors by exogenous agonists in rat cerebral cortex slices and synaptosomes

  1987cites this paper
• Methiothepin enhances the potassium-evoked release of [3H]-noradrenaline in rat pineal gland

  1987cites this paper
• Interaction between neuronal uptake inhibitors and presynaptic serotonin autoreceptors in rat hypothalamic slices: comparison of K+ and electrical depolarization.

  1987cites this paper
• Central serotonin receptors as targets for drug research.

  1987cites this paper
• Autoreceptors in the central nervous system

  1987cites this paper
• Effects of RU 24969 on serotonin release in rat brain cortex: further support for the identity of serotonin autoreceptors with 5-HT1B sites.

  1987cites this paper
• Influence of eicosanoids on serotonin release in the rat brain: inhibition by prostaglandins E1 and E2

  1987cites this paper
• Different Presynaptic Receptors Modulate Neuronal Uptake and Transmitter Release in Serotoninergic Nerve Terminals

  1987cites this paper
• Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin

  1987cites this paper
• Proceedings of the British Pharmacological Society. 18th-20th December 1985. Abstracts.

  1986cites this paper
• Serotonin uptake inhibitors and the prejunctional effects of serotonin on peripheral sympathetic nerves.

  1986cites this paper
• Recent advances in central 5-hydroxytryptamine receptor agonists and antagonists.

  1986cites this paper
• Studies on the Role of α2‐Adrenoceptors in the Control of Synaptosomal [3H]5‐Hydroxytryptamine Release: Effects of Antidepressant Drugs

  1986cites this paper
• Neurobiology of an anorectic drug: fenfluramine.

  1986cites this paper
• Effects of a selective 5-HT reuptake blocker, citalopram, on the sensitivity of 5-HT autoreceptors: Electrophysiological studies in the rat brain

  1986cites this paper
• Presynaptic 5-HT autoreceptors and the modulation of the release of 5-HT.

  1986cites this paper
• A simple organ bath for electrical stimulation and superfusion of rat brain slices.

  1986cites this paper
• Chapter 5. Drugs Acting at Central 5-Hydroxytryptamine Receptors

  1986cites this paper
• In vivo electrophysiological evidence for the regulatory role of autoreceptors on serotonergic terminals

  1986cites this paper
• Serotonin neurochemistry revisited: A new look at some old axioms.

  1986cites this paper
• Autoreceptors and α2-adrenoceptors at the serotonergic axons of rabbit brain cortex

  1986cites this paper
• Dihydroergocristine-induced stimulation of the 5-HT autoreceptor in the hypothalamus of the rat.

  1986cites this paper
• Neurochemical mechanism of action of drugs which modify feeding via the serotoninergic system.

  1986cites this paper
• Autoreceptors and alpha 2-adrenoceptors at the serotonergic axons of rabbit brain cortex.

  1986cites this paper
• Effect of vasoactive intestinal peptide on serotonin metabolism in the suprachiasmatic area of the rat: mechanism of action.

  1986cites this paper
• Stimulation of the Serotonin Autoreceptor Prevents the Calcium‐Calmodulin‐Dependent Increase of Serotonin Biosynthesis in Rat Raphe Slices

  1986cites this paper