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Titolo:
CHARACTERIZATION OF [I-125] -2-[N-PROPYL-N-(3'-IODO-2'-PROPENYL)AMINO]TETRALIN BINDING TO DOPAMINE D3 RECEPTORS IN RAT OLFACTORY TUBERCLE
Autore:
BURRIS KD; FLITZ TM; CHUMPRADIT S; KUNG MP; FOULON C; HENSLER JG; KUNG HF; MOLINOFF PB;
Indirizzi:
UNIV PENN,SCH MED,DEPT PHARMACOL PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104 UNIV PENN,DEPT PSYCHIAT PHILADELPHIA PA 19104
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 2, volume: 268, anno: 1994,
pagine: 935 - 942
SICI:
0022-3565(1994)268:2<935:CO[->2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
AUTORADIOGRAPHIC LOCALIZATION; SEROTONIN RECEPTORS; PITUITARY-CELLS; H-3 QUINPIROLE; HIGH-AFFINITY; BRAIN; PROTEINS; AGONISTS; INHIBITION; NUCLEOTIDE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
K.D. Burris et al., "CHARACTERIZATION OF [I-125] -2-[N-PROPYL-N-(3'-IODO-2'-PROPENYL)AMINO]TETRALIN BINDING TO DOPAMINE D3 RECEPTORS IN RAT OLFACTORY TUBERCLE", The Journal of pharmacology and experimental therapeutics, 268(2), 1994, pp. 935-942

Abstract

,S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-prop penyl)-amino]tetralin ([(125)](R,S)-trans-7-OH-PIPAT been shown to bind with high affinity to dopamine D3 receptors expressed in Spodoptera frugiperda cells. No specific binding was seen in Spodoptera frugiperda cells expressinga high density of D2 receptors. It was therefore, suggested that [I-125] (R,S)-trans-7-OH-PIPAT selectively labels D3 receptors. In the present study, saturation binding of [I-125](R)-trans-7-OH-PIPAT to membranes from rat olfactory tubercle resulted in markedly curvilinear Scatchard plots, suggesting that the radioligand was binding to more than one receptor class or affinity state. [I-125] (R)-trans-7-OH-PIPAT bound with high affinity to membranes from human embryonic kidney-293 cells expressing transfected D2 or D3 receptors and to membranes from Chinese hamster ovary cells expressing serotonin(1A) receptors. Binding of [I-125](R)- trans-7-OH-PIPAT to serotonin(1A), and D2 receptors was decreased or eliminated in the presence of NaCl and/or guanylyl-imidodiphosphate [Gpp(NH)p]. In the presence of Gpp(NH)p and NaCl, a linear Scatchard plot with a K-d value of 0.4 nM and a density of 100 fmol/mgof protein was obtained in membranes from rat olfactory tubercle. Agonists and antagonists inhibited binding of [I-125](R)-trans-7-OH-PIPATwith a rank order of potency consistent with an interaction at D3 receptors. These results suggest that, in the presence of Gpp(NH)p and NaCl, [I-125](R)-trans-7-OH-PIPAT specifically labels D3 receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 01:17:40