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Titolo:
F-18 LABELED BENZAMIDES FOR STUDYING THE DOPAMINE-D(2) RECEPTOR WITH POSITRON EMISSION TOMOGRAPHY
Autore:
MACH RH; LUEDTKE RR; UNSWORTH CD; BOUNDY VA; NOWAK PA; SCRIPKO JG; ELDER ST; JACKSON JR; HOFFMAN PL; EVORA PH; RAO AV; MOLINOFF PB; CHILDERS SR; EHRENKAUFER RL;
Indirizzi:
BOWMAN GRAY SCH MED,DEPT RADIOL,MED CTR BLVD WINSTON SALEM NC 27157 UNIV PENN,CEREBROVASC RES CTR PHILADELPHIA PA 19104 UNIV PENN,DEPT PHARMACOL PHILADELPHIA PA 19104 WAKE FOREST UNIV,BOWMAN GRAY SCH MED,DEPT PHYSIOL & PHARMACOL WINSTONSALEM NC 27157
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 23, volume: 36, anno: 1993,
pagine: 3707 - 3720
SICI:
0022-2623(1993)36:23<3707:FLBFST>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIVING HUMAN-BRAIN; RAT-BRAIN; H-3 RACLOPRIDE; HIGH-AFFINITY; SUBSTITUTED BENZAMIDE; ENDOGENOUS DOPAMINE; ANTIPSYCHOTIC AGENTS; PARKINSONS-DISEASE; BINDING-PROPERTIES; INVITRO BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
65
Recensione:
Indirizzi per estratti:
Citazione:
R.H. Mach et al., "F-18 LABELED BENZAMIDES FOR STUDYING THE DOPAMINE-D(2) RECEPTOR WITH POSITRON EMISSION TOMOGRAPHY", Journal of medicinal chemistry, 36(23), 1993, pp. 3707-3720

Abstract

Two series of (N-benzylpiperidin-4-yl)- and (9-azabicyclo[3.3.1]nonan-3beta-yl)benzamides were prepared, and in vitro binding assays were used to measure the affinity of these compounds for dopamine D2, dopamine D3, serotonin 5-HT2, and alpha2-adrenergic receptors. The results of these studies indicated compounds 23, 26b, and 34 have the selectivity needed for in vivo studies of the D2 (and possibly D3) receptors. F-18-Labeled analogues of 23, 26b and 34 were prepared by N-alkylation of the corresponding desbenzyl precursors with [F-18]-4-fluorobenzyl iodide. Preliminary in vivo studies demonstrated that [F-18]-23 and [F-18]-26b are suitable candidates for further evaluation in positron emission tomography imaging studies. The slow rate of washout of [F-18]-34 from nondopaminergic regions and its comparatively high lipophilicity indicates that this compound may not be suitable for imaging studiesbecause of a high level of nonspecific binding.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/01/20 alle ore 00:57:11