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Titolo:
SYNTHESIS AND OPTICAL RESOLUTION OF (R)- AND -2-[N-PROPYL-N-(3'-IODO-2'-PROPENYL)AMINO]TETRALIN - A NEW D3 DOPAMINE-RECEPTOR LIGAND
Autore:
CHUMPRADIT S; KUNG MP; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,3700 MARKET ST,RM 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: 36, anno: 1993,
pagine: 4308 - 4312
SICI:
0022-2623(1993)36:26<4308:SAORO(>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
MOLECULAR-CLONING; GENE; EXPRESSION; D1; NEUROLEPTICS; LOCALIZATION; TARGET; AGENT; CDNA;
Tipo documento:
Note
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
S. Chumpradit et al., "SYNTHESIS AND OPTICAL RESOLUTION OF (R)- AND -2-[N-PROPYL-N-(3'-IODO-2'-PROPENYL)AMINO]TETRALIN - A NEW D3 DOPAMINE-RECEPTOR LIGAND", Journal of medicinal chemistry, 36(26), 1993, pp. 4308-4312

Abstract

An improved method for synthesis and resolution of -hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino] tetralin (trans-7-OH-PlPAT, 5), a newD3 dopamine receptor ligand, was reported. Both isomers, (R)-(+)- and(S)-(-)-5, were prepared and characterized. HPLC retention times obtained on a chiral column for these isomers were consistent with those observed for [I-125]-(R)-(+)- and (S)-(-)-5. Direct radioiodination of an optically resolved tin precursor, (R)-(+)-7, yielded the desired [I-125](R)-(+)-5, which is a simpler method for synthesis of this ligand. Binding studies with membrane preparations containing D3 dopamine receptors expressed in Spodoptera frugiperda (Sf9) cells also suggested that the [I-125](R)-(+)-5 is the active isomer (K-d = 0.05 nM). The schemes described may provide an efficient way for synthesizing a large quantity of this new D3 dopamine receptor ligand for in vivo behavior studies.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/01/20 alle ore 01:20:15