SYNTHESIS OF [H-3] NALTRINDOLE

被引：12

作者：

DORN, CR ^{[1
]}

MARKOS, CS ^{[1
]}

DAPPEN, MS ^{[1
]}

PITZELE, BS ^{[1
]}

机构：

[1] SEARLE RES & DEV DIV, DEPT MED CHEM, SKOKIE, IL 60077 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1992年 / 31卷 / 05期

关键词：

TRITIUM; NALTRINDOLE; CATALYTIC TRITIOLYSIS; DELTA OPIOID RECEPTOR LIGAND;

D O I：

10.1002/jlcr.2580310506

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

[H-3]Naltrindole ([H-3] 1) was prepared for use as a selective radiolabeled ligand for delta opioid receptors. The Fischer indole synthesis from naltrexone and 2,4-dibromophenylhydrazine produced dibromide precursor 2, which was catalytically dehalogenated with carrier free tritium gas to afford [H-3] 1 in 45.8% yield at a specific activity of 39.5 Ci/mmol.

引用

页码：375 / 380

页数：6

共 5 条

[1]

DORN CR, 1991, 4TH CENTR US DIV M I

[2] APPLICATION OF THE MESSAGE ADDRESS CONCEPT IN THE DESIGN OF HIGHLY POTENT AND SELECTIVE NON-PEPTIDE DELTA-OPIOID RECEPTOR ANTAGONISTS [J].

PORTOGHESE, PS ;

SULTANA, M ;

NAGASE, H ;

TAKEMORI, AE .

JOURNAL OF MEDICINAL CHEMISTRY, 1988, 31 (02) :281-282

[3] DESIGN OF PEPTIDOMIMETIC DELTA-OPIOID RECEPTOR ANTAGONISTS USING THE MESSAGE ADDRESS CONCEPT [J].

PORTOGHESE, PS ;

SULTANA, M ;

TAKEMORI, AE .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (06) :1714-1720

[4] NALTRINDOLE, A HIGHLY SELECTIVE AND POTENT NON-PEPTIDE-DELTA OPIOID RECEPTOR ANTAGONIST [J].

PORTOGHESE, PS ;

SULTANA, M ;

TAKEMORI, AE .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 146 (01) :185-186

[5]

SOFUOGLU M, 1991, J PHARMACOL EXP THER, V257, P676

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