Linked Life Data

15363660

Source:http://linkedlifedata.com/resource/pubmed/id/15363660

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
21
pubmed:dateCreated
2004-9-14
pubmed:abstractText
Even though conventional systemic doses of cimetidine and other histamine H(2) antagonists display minimal brain penetration, central nervous system (CNS) effects (including seizures and analgesia) have been reported after administration of these drugs in animals and man. To test the hypothesis that cimetidine-like drugs produce these CNS effects via inhibition of GABA(A) receptors, the actions of these drugs were studied on seven different, precisely-defined rat recombinant GABA(A) receptors using whole-cell patch clamp recordings. The H(2) antagonists famotidine and tiotidine produced competitive and reversible inhibition of GABA-evoked currents in HEK293 cells transfected with various GABA(A) receptor subunits (IC(50) values were between 10-50 microM). In contrast, the H(2) antagonist ranitidine and the cimetidine congener improgan had very weak (if any) effects (IC(50) > 50 microM). Since the concentrations of cimetidine-like drugs required to inhibit GABA(A) receptors in vitro (greater than 50 microM) are considerably higher than those found during analgesia and/or seizures (1-2 microM), the present results suggest that cimetidine-like drugs do not appear to produce seizures or analgesia by directly inhibiting GABA(A) receptors.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0024-3205
pubmed:author
pubmed:issnType
Print
pubmed:day
8
pubmed:volume
75
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2551-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
Effects of cimetidine-like drugs on recombinant GABAA receptors.
pubmed:affiliation
Center for Neuropharmacology and Neuroscience, Albany Medical College MC-136, 47 New Scotland Ave., Albany, NY 12206, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.