Linked Life Data

9225290

Source:http://linkedlifedata.com/resource/pubmed/id/9225290

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4-5
pubmed:dateCreated
1997-9-15
pubmed:abstractText
Potentiation of the 5-HT3 receptor-mediated ion current in mouse N1E-115 neuroblastoma cells by 5-hydroxyindole (5-OHi) and three analogues (5-aminoindole, catechol and indole) was examined using whole-cell voltage clamp and single channel patch clamp techniques. The substances tested enhanced the amplitude of the maximum 5-HT-evoked ion current by 12-30%. The rank order (at 1 mM) to potentiate the 5-HT-induced current was: 5-OHi approximately 5-aminoindole approximately catechol > indole. The concentration-effect curve of 5-HT was shifted leftwards by 1 mM 5-OHi, resulting in a two-fold increase of the apparent affinity of 5-HT from 1.4 microM to 0.7 microM, without affecting the Hill coefficient. The time constant of reversal of activation of the 5-HT-induced ion current upon washout of the agonist was delayed by 1 mM 5-OHi from 4.0 sec to 12.8 sec. 5-HT3 receptor-gated single channel events in cell-attached patches in the presence and absence of 1 mM 5-OHi were indistinguishable, apart from a slight increase in the event frequency. The results suggest that 5-OHi and analogues potentiate the 5-HT3 receptor-mediated ion current by delaying agonist dissociation and thereby increase the probability of channel opening. From the increased apparent affinity of 5-HT and the non-surmountability of the potentiating effect, it is concluded that 5-OHi and analogues are allosteric modulators of 5-HT3 receptors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0028-3908
pubmed:author
pubmed:issnType
Print
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
649-53
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed:articleTitle
Allosteric potentiation of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells by 5-hydroxyindole and analogues.
pubmed:affiliation
Research Institute of Toxicology, Utrecht University, The Netherlands.
pubmed:publicationType
Journal Article