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Titolo:
A POTENTIAL 5-HT1A RECEPTOR ANTAGONIST - P-MPPI
Autore:
KUNG HF; KUNG MP; CLARKE W; MAAYANI S; ZHUANG ZP;
Indirizzi:
UNIV PENN,DEPT RADIOL,ROOM 305,3700 MARKET ST PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104 CUNY MT SINAI SCH MED,DEPT PHARMACOL NEW YORK NY 10029 CUNY MT SINAI SCH MED,DEPT ANESTHESIOL NEW YORK NY 10029
Titolo Testata:
Life sciences
fascicolo: 19, volume: 55, anno: 1994,
pagine: 1459 - 1462
SICI:
0024-3205(1994)55:19<1459:AP5RA->2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSTSYNAPTIC 5-HT(1A) RECEPTORS; SELECTIVE ANTAGONIST; AFFINITY; LIGAND;
Keywords:
5-HT1A RECEPTOR; LIGAND BINDING; [I-125] P-MPPI;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
14
Recensione:
Indirizzi per estratti:
Citazione:
H.F. Kung et al., "A POTENTIAL 5-HT1A RECEPTOR ANTAGONIST - P-MPPI", Life sciences, 55(19), 1994, pp. 1459-1462

Abstract

A potential 5-HT1A receptor antagonist, p-MPPI, -2''-pyridinyl)-p-iodobenzamido-]ethyl-piperazine, was developed. The [I-125]p-MPPI demonstrated high affinity and selectivity toward 5-HT1A receptors; K-d = 0.36 nM and B-max = 264 fmol/mg of protein in rat hippocampal membrane homogenates. The binding is not sensitive to GTP (300 mu M) or Gpp(NH)p (100 mu M) In forskolin-stimulated adenylyl cyclase assay using rat hippocampus, p-MPPI (up to 10 mu M) showed no agonist activity as compared to that of (+/-)-X-OH-DPAT. At 100 nM it completely antagonized theinhibition of forskolin-stimulated adenylyl cyclase activity producedby 100 nM of (+/-)-8-OH-DPAT. This potential 5-HT1A antagonist may provide a powerful tool for studies of the pharmacology of the 5-HT1A receptor system.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 22:26:50