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Titolo:
CHARACTERIZATION OF A NOVEL IODINATED LIGAND, IPMPP, FOR HUMAN DOPAMINE D4 RECEPTORS EXPRESSED IN CHO CELLS
Autore:
KUNG MP; STEVENSON DA; ZHUANG ZP; VESSOTSKIE JM; CHUMPRADIT S; SUN XM; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104
Titolo Testata:
Life sciences
fascicolo: 2, volume: 60, anno: 1996,
pagine: 91 - 100
SICI:
0024-3205(1996)60:2<91:COANIL>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
HAMSTER OVARY CELLS; GUANOSINE-5'-O-(3-)S-35>THIO)TRIPHOSPHATE BINDING; INSECT CELLS; RAT-BRAIN; SCHIZOPHRENIA; MEMBRANES; AGONISTS; D-2;
Keywords:
RADIOIODINATED LIGAND; G PROTEIN-COUPLING; DOPAMINE D4 RECEPTORS; AGONIST; ANTAGONIST; HIGH-AFFINITY BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
M.P. Kung et al., "CHARACTERIZATION OF A NOVEL IODINATED LIGAND, IPMPP, FOR HUMAN DOPAMINE D4 RECEPTORS EXPRESSED IN CHO CELLS", Life sciences, 60(2), 1996, pp. 91-100

Abstract

A novel radioiodinated ligand with a high specific activity (2,200 Ci/mmol), iodophenyl)piperazin-1-yl]methyl-1H-pyrrolo(2,3-b) pyridine ([I-125]IPMPP), was successfully prepared. Binding characteristics of [I-125]IPMPP were evaluated using human dopamine D4 (D4.2 variant) receptors expressed in Chinese hamster ovary (CHO) cells. Saturation analysis revealed high affinity binding sites for [I-125]IPMPP (K-d = 0.39 +/- 0.18 nM). The number of D4 receptors labeled with [I-125]IPMPP at room temperature was four times higher than that labeled with [I-125]S(-)5-OH-PIPAT, a radioiodinated agonist ligand (572 fmol/mg protein vs.125 fmol/mg protein). A significant decrease in the number of bindingsites was observed with [I-125]S(-)5-OH-PIPAT when assays were carried out at a higher temperature (37 degrees C vs. 25 degrees C). In contrast to [I-125]S(-)5-OH-PIPAT, [I-125]IPMPP labeled more D4 sites at 37 degrees C. Neither magnesium ion nor guanylimidodiphosphate (Gpp(NH)p) affected [I-125]IPMPP binding. These data support the conclusion that [I-125]IPMPP is an antagonist ligand. The potency of various compounds, including clozapine, to inhibit [I-125]IPMPP binding is consistent with the rank order measured with other radioligands for D4 receptors. In addition, measuring D4 receptor stimulation of [S-35]GTP gamma Sbinding further demonstrated the antagonist property of IPMPP.

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Documento generato il 25/01/20 alle ore 19:46:45