Linked Life Data

2552425

Source:http://linkedlifedata.com/resource/pubmed/id/2552425

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
1989-10-28
pubmed:abstractText
In this investigation an attempt was made to evaluate quantitatively the relationship between benzodiazepine receptor occupancy and the anticonvulsant effect of flunitrazepam in rats. A graded measure of anticonvulsant effect was obtained on the basis of an elevation of pentylenetetrazol (PTZ) threshold concentrations. The concentration-anticonvulsant effect relationship could be described by the Emax model with an EC50 in cerebrospinal fluid of 2.9 +/- 0.8 micrograms/liter and an Emax of 227 +/- 22 mg/liter PTZ (mean +/- SE). In vitro receptor occupancy was determined in a crude brain homogenate at 0 and 37 degrees C, which yielded KD values of 2.2 +/- 0.2 and 26 +/- 2 micrograms/liter, respectively. The results obtained in both experiments were combined by focusing on free flunitrazepam concentrations. This strategy resulted in a nonlinear relationship between receptor occupancy and anticonvulsant effect of flunitrazepam, with 90% of the maximum response achieved at a degree of receptor occupancy of approximately 50% at 37 degrees C.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0724-8741
pubmed:author
pubmed:issnType
Print
pubmed:volume
6
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
585-91
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Relationship between receptor occupancy at 37 degrees C and the anticonvulsant effect of flunitrazepam in rats.
pubmed:affiliation
Division of Pharmacology, University of Leiden, The Netherlands.
pubmed:publicationType
Journal Article