Linked Life Data

9257944

Source:http://linkedlifedata.com/resource/pubmed/id/9257944

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
1997-10-21
pubmed:abstractText
Recently, [125I]S(-)5-OH-PIPAT [5-hydroxy-2-(N-n-propyl-N-3'-iodo-2'-propenyl)aminotetralin], a derivative of S(-)5-OH-DPAT (5-hydroxy-N,N-di-n-propyl-aminotetralin), was reported to be a better radioiodinated dopamine D2-like receptor ligand than the previously reported iodinated ligand, [125I]R(+)7-OH-PIPAT. Therefore, in the present study, the binding profile of [125I]S(-)5-OH-PIPAT to D2-like receptors expressed in cell lines was established. High binding affinity (Kd = 0.3-0.4 nM) and NaCl sensitivity were displayed with this ligand in membranes of human embryonic kidney (HEK293) cells expressing either human D2 or rat D3 receptors and in Chinese hamster ovary (CHO) cells expressing human dopamine D4 receptors. Specific binding to D2 and D4 receptors was significantly increased in the presence of 2 mM MgCl2 and decreased in the presence of 100 microM 5'-guanylyl-imidodiphosphate (GMP-PNP). This finding is consistent with reports that 2-aminotetralin compounds display agonist properties. The specific binding to D3 receptors however, was not affected by either MgCl2 or GMP-PNP. This lack of GMP-PNP sensitivity for D3 receptors may result from inadequate G protein-receptor coupling in this cell line. The rank order of potency for inhibition of [125I]S(-)5-OH-PIPAT binding with various dopamine agents was consistent with reported values for D2, D3 and D4 receptors. In membranes prepared from Spodoptera frugiperda (Sf9) cells infected with baculovirus that contains DNA encoding D3 receptors, [125I]S(-)5-OH-PIPAT recognized only 70% of the receptor population labeled by [125I]NCQ298. This new ligand offers several unique advantages, including high specific activity, high binding affinity and selectivity for D2-like receptors, that make it an excellent probe for the investigation and the characterization of dopamine D2-like receptors.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0028-3908
pubmed:author
pubmed:issnType
Print
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
999-1007
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Characterization of [125I]S(-)5-OH-PIPAT binding to dopamine D2-like receptors expressed in cell lines.
pubmed:affiliation
Department of Pharmacology, University of Pennsylvania, Philadelphia 19104, USA. jvess@sunmac.spect.upenn.edu
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.