Linked Life Data

10700661

Source:http://linkedlifedata.com/resource/pubmed/id/10700661

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2000-5-1
pubmed:abstractText
The serotonin 5-hydroxytryptamine-1A (5-HT(1A)) receptor subtype is of central interest in research, particularly in the area of pathophysiology and pharmacological treatment of psychiatric disorders. Robalzotan (generic name for NAD-299) is a new putative drug that binds with high selectivity and affinity to 5-HT(1A)-receptors in the rodent brain in vitro and in vivo. The aim of this positron emission tomography study was to determine 5-HT(1A) receptor occupancy in the cynomolgus monkey brain in vivo after IV injection of robalzotan. Two healthy monkeys were examined with Positron Emission Tomography (PET) and the radioligand [carbonyl-(11)C]WAY-100635, the first after IV administration of 2 microg/kg and 20 microg/kg, and the second after 10 microg/kg and 100 microg/kg IV. 5-HT(1A) receptor occupancy was calculated using an equilibrium-ratio analysis. Robalzotan occupied 5-HT(1A) receptors in a dose-dependent and saturable manner. The highest 5-HT(1A) receptor occupancy (70-80%) was attained after 100 microg/kg. The relationship between robalzotan drug concentration and 5-HT(1A) receptor occupancy could be described by a hyperbolic function, which can be used to guide the selection of appropriate doses for the initial studies in man. The study further corroborates that quantitative neuroimaging of receptor binding has potentials for the evaluation and dose finding of new CNS drugs.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0893-133X
pubmed:author
pubmed:issnType
Print
pubmed:volume
22
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
422-9
pubmed:dateRevised
2011-5-18
pubmed:meshHeading
pubmed:year
2000
pubmed:articleTitle
PET-Determination of robalzotan (NAD-299) induced 5-HT(1A) receptor occupancy in the monkey brain.
pubmed:affiliation
Karolinska Institutet, Stockholm, Sweden.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't