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Titolo:
DERIVATIVES OF -(N-2''-PYRIDINYL-P-IODOBENZAMIDO)ETHYL]PIPERAZINE (P-MPPI) AS 5-HT1A LIGANDS
Autore:
ZHUANG ZP; KUNG MP; CHUMPRADIT S; MU M; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,ROOM 305 PHILADELPHIA PA 19104 UNIV PENN,DEPT RADIOL PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 26, volume: 37, anno: 1994,
pagine: 4572 - 4575
SICI:
0022-2623(1994)37:26<4572:DO-(>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSTSYNAPTIC 5-HT(1A) RECEPTORS; BINDING-SITES; RAT-BRAIN; SELECTIVE ANTAGONIST; RADIOLIGAND; AFFINITY; NAN-190; INVITRO;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
Z.P. Zhuang et al., "DERIVATIVES OF -(N-2''-PYRIDINYL-P-IODOBENZAMIDO)ETHYL]PIPERAZINE (P-MPPI) AS 5-HT1A LIGANDS", Journal of medicinal chemistry, 37(26), 1994, pp. 4572-4575

Abstract

A series of new p-alkylbenzamido derivatives of N-2''-pyridinyl)-p-iodobenzamido)ethyl]piperazines (p-MPPI) were prepared. In vitro bindingstudies suggest that p-methyl and p-ethyl substituents on the benzamido group display the same high binding affinity to 5-HT1A receptors (K-i = 2.2 and 9.3 nM, rat hippocampal homogenates). However, when the substitution groups were larger than a C-5 pentyl group, the affinity to 5-HT1A receptors dropped below a useful level (K-i > 50 nM). Severalirreversible binding agents (CH2Cl, NHCOCH2Cl) and a photoaffinity, labeling compound (m-iodo p-azido) which showed good binding affinity to 6-HT1A receptors were successfully prepared.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 01:01:37