BIOMAT Database Logo BIOMAT Database Logo

Release of serotonin induced by 3,4-methylenedioxymethamphetamine (MDMA) and other substituted amphetamines in cultured fetal raphe neurons: further evidence for calcium-independent mechanisms of release. 1995

C H Wichems, and C K Hollingsworth, and B A Bennett
Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC 27157-1083, USA.

The substituted amphetamines 3,4-methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxyamphetamine (MDA), p-chloro-amphetamine (PCA) and fenfluramine (FEN) all exert their effects by releasing serotonin (5-HT) from presynaptic nerve terminals. In the current study, we examined the ability of these agents to induce the release of 5-HT in culture fetal raphe neurons. The data indicate that the rank order of release potencies for these agents was (+/-)PCA>(+)MDMA=(+)MDA=(+/-)FEN. Studies examining the role fo calcium in 5-HT release demonstrate that preventing calcium influx with L- and N-type calcium channel blockers inhibits potassium-stimulated release of -3H-5-HT but has no effect on release induced by the substituted amphetamines. Furthermore, omitting calcium from the extracellular media or depleting the vesicular pool of neurotransmitter with continual potassium stimulation did not affect the release of -3H-5-HT induced by these compounds. Administration of fluoxetine prior to the substituted amphetamines significantly attenuated the releasing effects of these agents, while producing no effect on potassium-stimulated release. These results are consistent with the notion that the amphetamines induce release of cytoplasmic 5-HT via the plasma membrane transporter.

UI MeSH Term Description Entries
D011189 Potassium Chloride A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA. Slow-K,Chloride, Potassium
D011903 Raphe Nuclei Collections of small neurons centrally scattered among many fibers from the level of the TROCHLEAR NUCLEUS in the midbrain to the hypoglossal area in the MEDULLA OBLONGATA. Caudal Linear Nucleus of the Raphe,Interfascicular Nucleus,Nucleus Incertus,Rostral Linear Nucleus of Raphe,Rostral Linear Nucleus of the Raphe,Superior Central Nucleus,Central Nucleus, Superior,Incertus, Nucleus,Nuclei, Raphe,Nucleus, Interfascicular,Nucleus, Raphe,Nucleus, Superior Central,Raphe Nucleus
D002118 Calcium A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes. Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005277 Fenfluramine A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release. Fintepla,Fenfluramine Hydrochloride,Fenfluramine Hydrochloride, (+-)-Isomer,Fenfluramine Hydrochloride, R-Isomer,Fenfluramine, (+-)-Isomer,Fenfluramine, R-Isomer,Isomeride,Pondimin,Fenfluramine Hydrochloride, R Isomer,Fenfluramine, R Isomer,Hydrochloride, Fenfluramine
D000661 Amphetamine A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE. Desoxynorephedrin,Levoamphetamine,Phenopromin,l-Amphetamine,Amfetamine,Amphetamine Sulfate,Amphetamine Sulfate (2:1),Centramina,Fenamine,Mydrial,Phenamine,Thyramine,levo-Amphetamine,Sulfate, Amphetamine,l Amphetamine,levo Amphetamine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012701 Serotonin A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator. 5-HT,5-Hydroxytryptamine,3-(2-Aminoethyl)-1H-indol-5-ol,Enteramine,Hippophaine,Hydroxytryptamine,5 Hydroxytryptamine
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

Related Publications

C H Wichems, and C K Hollingsworth, and B A Bennett
MDMA (3,4-methylenedioxymethamphetamine) inhibits the firing of dorsal raphe neurons in brain slices via release of serotonin.
August 1989, European journal of pharmacology,
C H Wichems, and C K Hollingsworth, and B A Bennett
3,4-methylenedioxymethamphetamine (MDMA)-induced release of endogenous serotonin from the rat dorsal raphe nucleus in vitro: Effects of fluoxetine and tryptophan.
January 1990, Neurochemistry international,
C H Wichems, and C K Hollingsworth, and B A Bennett
Evidence for a common mechanism of serotonin release induced by substituted amphetamines in vitro.
May 1992, Annals of the New York Academy of Sciences,
C H Wichems, and C K Hollingsworth, and B A Bennett
3,4-Methylenedioxymethamphetamine (MDMA) and other amphetamine derivatives.
March 1988, Journal of forensic sciences,
C H Wichems, and C K Hollingsworth, and B A Bennett
3,4-Methylenedioxymethamphetamine-induced release of serotonin and inhibition of dorsal raphe cell firing: potentiation by L-tryptophan.
March 1990, European journal of pharmacology,
C H Wichems, and C K Hollingsworth, and B A Bennett
Loss of serotonin transporter protein after MDMA and other ring-substituted amphetamines.
December 2006, Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology,
C H Wichems, and C K Hollingsworth, and B A Bennett
Glucocorticoids and 3,4-methylenedioxymethamphetamine (MDMA)-induced neurotoxicity.
February 1989, European journal of pharmacology,
C H Wichems, and C K Hollingsworth, and B A Bennett
Effect of 3,4-methylenedioxymethamphetamine (MDMA) on hippocampal dopamine and serotonin.
December 1998, Pharmacology, biochemistry, and behavior,
C H Wichems, and C K Hollingsworth, and B A Bennett
Mechanisms and environmental factors that underlying the intensification of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy)-induced serotonin syndrome in rats.
April 2015, Psychopharmacology,
C H Wichems, and C K Hollingsworth, and B A Bennett
Hypothyroidism alters striatal dopamine release mediated by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy).
April 2006, Synapse (New York, N.Y.),
Copied contents to your clipboard!