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Titolo:
(N-2''-PYRIDINYL)-P-IODOBENZAMIDO]ETHYL-PIPERAZINE ([I-125]P-MPPI) ASA NEW SELECTIVE RADIOLIGAND OF SEROTONIN-1A SITES IN RAT-BRAIN - IN-VITRO BINDING AND AUTORADIOGRAPHIC STUDIES
Autore:
KUNG MP; FREDERICK D; MU M; ZHUANG ZP; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 272, anno: 1995,
pagine: 429 - 437
SICI:
0022-3565(1995)272:1<429:((A>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSTSYNAPTIC 5-HT(1A) RECEPTORS; DORSAL RAPHE NUCLEUS; 5-HT1A RECEPTORS; GUINEA-PIG; RECIPROCAL MODULATION; HIPPOCAMPAL MEMBRANES; ANTAGONIST PROPERTIES; INTRINSIC ACTIVITY; G-PROTEINS; AGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
57
Recensione:
Indirizzi per estratti:
Citazione:
M.P. Kung et al., "(N-2''-PYRIDINYL)-P-IODOBENZAMIDO]ETHYL-PIPERAZINE ([I-125]P-MPPI) ASA NEW SELECTIVE RADIOLIGAND OF SEROTONIN-1A SITES IN RAT-BRAIN - IN-VITRO BINDING AND AUTORADIOGRAPHIC STUDIES", The Journal of pharmacology and experimental therapeutics, 272(1), 1995, pp. 429-437

Abstract

Binding characteristics of a radioiodinated serotonin-1A (5-HT1A) receptor antagonist, n-2''-pyridinyl)-p-iodobenzamido]-ethyl-piperazine ([I-125]p-MPPI) were evaluated using in vitro homogenate binding and autoradiographic techniques in rat brains. [I-125]p-MPPI displayed a K-dvalue of 0.32 +/- 0.04 nM (in the presence of MgCl2) and a B-max value of 315 +/- 60 fmol/mg of protein in rat hippocampal homogenates. Thenumber of 5-HT1A receptors labeled by [I-125]p-MPPI was 40% higher than that labeled by -2-(N-n-propyl-N-3'-iodo-2'-propenyl)aminotetralin ([I-125]R(+)8-OH-PIPAT) (225 +/- 47 fmol/mg of protein), a radioiodinated 5-HT1A agonist. The magnesium ion showed an inhibitory effect on [I-125]p-MPPI binding but increased the specific binding of [I-125]R(+)8-OH-PIPAT. A significant increase in B-max values in the presence of guanyl nucleotides was observed for [I-125]p-MPPI (control, 307 +/- 35fmol/mg of protein; with GTP, 345 +/- 30 fmol/mg of protein; with guanylyl-imidodiphosphate, 362 +/- 35 fmol/mg of protein); however, both guanyl nucleotides significantly reduced the B-max values measured by [I-125]R(+)8-OH-PIPAT (control, 213 +/- 50 fmol/mg of protein; with GTP, 133 +/- 20 fmol/mg of protein; with guanylyl-imidodiphosphate, 108 /- 20 fmol/mg of protein). The binding characteristics of [I-125]p-MPPI for 5-HT1A receptors suggest that p-MPPI is an antagonist for 5-HT1A receptors. In vitro autoradiographic studies in rat brain sections with [I-125]p-MPPI showed specific labeling of areas rich in 5-HT1A receptors and the regional distribution closely matched those labeled by [I-125]R(+)8-OH-PIPAT. This novel radioiodinated compound, [I-125]p-MPPI, is the first selective 5-HT1A receptor ligand reported in the literature. Together with the agonist radioligand, [I-125]R(+)8-OH-PIPAT, these two ligands may provide useful tools for studies of 5-HT1A receptors in the central nervous system.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/06/20 alle ore 01:58:05