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Titolo:
CHARACTERIZATION OF [I-125] S(-)5-OH-PIPAT BINDING TO DOPAMINE D-2-LIKE RECEPTORS EXPRESSED IN CELL-LINES
Autore:
VESSOTSKIE JM; KUNG MP; CHUMPRADIT S; KUNG HF;
Indirizzi:
UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104
Titolo Testata:
Neuropharmacology
fascicolo: 7, volume: 36, anno: 1997,
pagine: 999 - 1007
SICI:
0028-3908(1997)36:7<999:CO[SBT>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
INFECTED INSECT CELLS; FUNCTIONAL-CHARACTERIZATION; HIGH-AFFINITY; RAT-BRAIN; LIGAND-BINDING; IMAGING AGENT; D3 RECEPTORS; D-2; D2; AGONISTS;
Keywords:
DOPAMINE D-2 RECEPTOR; DOPAMINE D-3 RECEPTOR; DOPAMINE D-4 RECEPTOR; RADIOLIGAND; AGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
44
Recensione:
Indirizzi per estratti:
Citazione:
J.M. Vessotskie et al., "CHARACTERIZATION OF [I-125] S(-)5-OH-PIPAT BINDING TO DOPAMINE D-2-LIKE RECEPTORS EXPRESSED IN CELL-LINES", Neuropharmacology, 36(7), 1997, pp. 999-1007

Abstract

Recently, [I-125]S(-)5-OH-PIPAT -(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 D-2-like receptor ligand than the previously reported iodinated ligand,[I-125]R(+)7- OH-PIPAT. Therefore, in the present study, the binding profile of [I-125]S(-)5-OH-PIPAT to D-2-like receptors expressed in cell lines was established. High binding affinity (K-d = 0.3-0.4 nM) andNaCl sensitivity were displayed with this ligand in membranes of human embryonic kidney (HEK293) cells expressing either human D-2 or rat D-3 receptors and in Chinese hamster ovary (CHO) cells expressing humandopamine D-4 receptors. Specific binding to D-2 and D-4 receptors wassignificantly increased in the presence of 2 mM MgCl2 and decreased in the presence of 100 mu M 5'-guanylyl-imidodiphosphate (GMP-PNP). This finding is consistent with reports that 2-aminotetralin compounds display agonist properties. The specific binding to D-3 receptors however, was not affected by either MgCl2 or GMP-PNP. This lack of GMP-PNP sensitivity for D-3 receptors may result from inadequate G protein-receptor coupling in this cell Line. The rank order of potency for inhibition of [I-125]S(-)5-OH-PIPAT binding with various dopamine agents was consistent with reported values for D-2, D-3 and D-4 receptors. In membranes prepared from Spodoptera frugiperda (Sf9) cells infected with baculovirus that contains DNA encoding D-3 receptors, [I-125]S(-)5-OH-PIPAT recognized only 70% of the receptor population labeled by [I-125]NCQ298. This new ligand offers several unique advantages, including high specific activity, high binding affinity and selectivity for D-2-like receptors, that make it an excellent probe for the investigation and the characterization of dopamine D-2-like receptors. (C) 1997 Elsevier Science Ltd.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 06:13:54