Linked Life Data

9048963

Source:http://linkedlifedata.com/resource/pubmed/id/9048963

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1997-4-1
pubmed:abstractText
Recently, a new imidazoline (I2) ligand, [3H]2-(2-benzofuranyl)-2-imidazoline (BFI) was shown to be more selective for I2 vs alpha 2 binding in rodent brain. We characterized [3H]BFI binding in human brain cortex and lateral reticular nucleus (NRL). Membranes were incubated with [3H]BFI at 22 degrees C in 50 mM Tris, 1.5 mM EDTA at pH 7.5. Saturation experiments with [3H]BFI (0.5-80 nM) were analyzed using non-linear curve fitting. The NRL had 4X more binding sites than cortex with similar affinity (Bmax = 2085 +/- 732 and 471 +/- 41 fmol/mg protein; KD = 9.3 +/- 3.5 and 11.9 +/- 2.7 nM, respectively). In competition studies, cortical [3H]BFI binding was displaced in order of decreasing potency by clorgyline > BFI > or = cirazoline > idazoxan > or = guanabenz > clonidine > RX821002. The monoamine oxidase (MAO) inhibitor tranylcypromine (TCP) (1 nM-10 microM), markedly enhanced [3H]BFI binding in both NRL and cortex. Enhanced binding was maximal at 300 nM (12 X control) and returned to baseline at 30 microM. Potentiation was not seen with pargyline or clorgyline. TCP did not effect [3H]BFI binding in rat cortex, or [3H]idazoxan binding in human cortex and NRL. In human cortex, inhibition of MAO by preincubation with pargyline (10 micro M) abolished the TCP effect. Upon preincubation with TCP, the stimulation of [3H]BFI binding was dose-dependently related to a simultaneous inhibition of MAO. Thus, [3H]BFI labels a site in human NRL and cortex that appears similar to the previously described I2 site labeled by [3H]idazoxan. However, [3H]BFI binding is dramatically stimulated by TCP in human brain via a mechanism dependent on endogenous MAO activity.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0024-3205
pubmed:author
pubmed:issnType
Print
pubmed:volume
60
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
605-15
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Binding of [3H]2-(2-benzofuranyl)-2-imidazoline (BFI) to human brain: potentiation by tranylcypromine.
pubmed:affiliation
Lilly Research Laboratories, Eli Lilly and Company Indianapolis, IN 46285, USA.
pubmed:publicationType
Journal Article, In Vitro