Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1988-4-22
pubmed:abstractText
The effect of midalcipran, an equipotent inhibitor of the uptake of 5-hydroxytryptamine (5-HT) and noradrenaline (NA), on the inhibition of release of 5-HT induced by lysergic acid diethylamide (LSD), was investigated by studying the overflow of transmitter from slices of hypothalamus from the rat prelabelled with [3H]5-HT. The (Z)-enantiomer of midalcipran, at 0.1 microM, displaced to the right the concentration-effect curve of inhibition of release of [3H]5-HT elicited by electrical stimulation induced by LSD. In contrast, the (E)-enantiomer, which does not inhibit the uptake of monoamines, was devoid of any antagonizing effect. The inhibitory effect of 0.1 microM LSD was not modified in the presence of maprotiline, bupropion or mianserin at 1 microM. The results of this study show that the interaction between the 5-HT autoreceptor and the inhibitors of the uptake of 5-HT is related exclusively to their potency at inhibiting the uptake of 5-HT. The effect of the monoamine oxidase inhibitor, pargyline (1-10 microM), was also studied on the field-stimulated release of [3H]5-HT. The inhibitory effect of this drug was antagonized by methiothepin at 0.1 and 1 microM, by phentolamine 1 microM and 10 microM and by the inhibitor of the uptake of 5-HT, citalopram at 0.1 and 1 microM. The action of pargyline appeared to be mediated through the activation of the serotonergic autoreceptor and of the presynaptic alpha-adrenoceptor located on serotonergic nerve terminals. The results obtained with pargyline are consistent with the hypothesis of an interaction between the 5-HT autoreceptor and the uptake site for 5-HT.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0028-3908
pubmed:author
pubmed:issnType
Print
pubmed:volume
27
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
43-9
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Sensitivity of the response of 5-HT autoreceptors to drugs modifying synaptic availability of 5-HT.
pubmed:affiliation
Department of Biochemical Pharmacology, Pierre Fabre Research Centre, Castres, France.
pubmed:publicationType
Journal Article, In Vitro