Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
A MALIGNANT-MELANOMA IMAGING AGENT - SYNTHESIS, CHARACTERIZATION, IN-VITRO BINDING AND BIODISTRIBUTION OF ODINE-125-(2-PIPERIDINYLAMINOETHYL)4-IODOBENZAMIDE
Autore:
JOHN CS; BOWEN WD; SAGA T; KINUYA S; VILNER BJ; BAUMGOLD J; PAIK CH; REBA RC; NEUMANN RD; VARMA VM; MCAFEE JG;
Indirizzi:
GEORGE WASHINGTON UNIV,MED CTR,RADIOPHARMACEUT CHEM SECT,662 ROSS HALL,2300 I ST NW WASHINGTON DC 20037 NIDDKDNM,MED CHEM LAB BETHESDA MD 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 12, volume: 34, anno: 1993,
pagine: 2169 - 2175
SICI:
0161-5505(1993)34:12<2169:AMIA-S>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
MONOCLONAL-ANTIBODY; RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
C.S. John et al., "A MALIGNANT-MELANOMA IMAGING AGENT - SYNTHESIS, CHARACTERIZATION, IN-VITRO BINDING AND BIODISTRIBUTION OF ODINE-125-(2-PIPERIDINYLAMINOETHYL)4-IODOBENZAMIDE", The Journal of nuclear medicine, 34(12), 1993, pp. 2169-2175

Abstract

In order to develop improved radiopharmaceuticals for imaging malignant melanoma, we have synthesized and characterized I-125- and I-131-labeled (2-piperidinylaminoethyl) 4-iodobenzamide (PAB). In vitro binding profiles of IPAB and N-(2-diethylaminoethyl) 4-iodobenzamide (IDAB, a structurally related analog of IPAB) for a variety of neurotransmitter receptors suggested that both IPAB and IDAB possessed a high sigma-1 affinity and a low affinity for sigma-e sites. In vitro homologous competition binding studies of [(125)l]PAB with human malignant melanoma cell A2058 showed that the tracer was bound to the cells with a highaffinity (Ki = 6.0 nM) and that the binding was saturable. Biodistribution studies in nude mice implanted with human malignant melanoma xenografts showed good tumor uptake (3.87% ID/g at 1 hr, 2.91% ID/g at 6 hr and 1.02% ID/g at 24 hr) of [(125)l]PAB. High tumor-to-nontarget organ ratios were obtained at 24 hr postinjection. Tumor-to-blood, liver, muscle, lung, intestines, heart and brain ratios at 24 hr were 17.80, 3.88, 94.58, 14.29, 10.87, 37.07 and 90.01, respectively. Tumor imaging with [I-131]PAB in a nude mice model xenografted with human malignant melanoma at 24 hr clearly delineated the tumor with very little activity in any other organ. These results demonstrate that sigma-1 receptors could be used as external markers for malignant melanoma.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 07:02:14