A SIMPLE METHOD FOR THE PREPARATION OF I-123 AND I-125 LABELED IODOBENZODIAZEPINES

被引：0
|
作者：
MCBRIDE, BJ [1 ]
BALDWIN, RM [1 ]
KERR, JM [1 ]
WU, JL [1 ]
机构：
[1] MEDIPHYS INC,EMERYVILLE,CA 94608
来源：
APPLIED RADIATION AND ISOTOPES | 1991年 / 42卷 / 02期
关键词：
D O I：
暂无
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
The tributyltin derivative of the benzodiazepine antagonist ethyl 7-iodo-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate (Ro 16-0154) was synthesized by a one-step Pd catalyzed reaction between bistributyltin and Ro 16-0154. Electrophilic iodination of the tributyltin compound with no-carrier-added I-125 and I-123 gave a 50-70% radiochemical yield of a greater than 98% radiochemically pure Ro 16-0154. The specific activity of [I-123]Ro 16-0154 and [I-125]Ro 16-0154 was 180,000 and 1700 Ci/mmol, respectively, but the effective specific activity was 6900 and 300 Ci/mmol due to the presence of benzodiazepine impurities which have similar receptor binding properties.
引用
收藏
页码：173 / 175
页数：3
相关论文
共 50 条
  • [41] Synthesis of [I-125/I-123]-IPH: A radiolabeled analog of epibatidine for in vivo studies of nicotinic acetylcholine receptors.
    Musachio, JL
    Scheffel, U
    Stathis, M
    Villemagne, V
    Finley, P
    Horti, A
    Kimes, A
    London, ED
    DavilaGarcia, M
    Kellar, KJ
    Dannals, RF
    JOURNAL OF NUCLEAR MEDICINE, 1996, 37 (05) : 12 - 12
  • [42] A NEW INTERMEDIATE FOR THE RAPID SYNTHESIS OF N-ISOPROPYL-P-(I-125)- OR P-(I-123) AMPHETAMINE
    PROTIVA, J
    KRECEK, V
    LESETICKY, L
    JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY-LETTERS, 1986, 107 (06): : 331 - 336
  • [43] EXCITATION-FUNCTIONS OF PROTON-INDUCED REACTIONS ON XE-126 - I-125 IMPURITY IN I-123
    VENIKOV, NI
    NOVIKOV, VI
    SEBIAKIN, AA
    APPLIED RADIATION AND ISOTOPES, 1993, 44 (04) : 751 - 754
  • [44] DNA DAMAGE PRODUCED IN V79 CELLS BY DNA-INCORPORATED I-123 - A COMPARISON WITH I-125
    MAKRIGIORGOS, GM
    BERMAN, RM
    BARANOWSKAKORTYLEWICZ, J
    BUMP, E
    HUMM, JL
    ADELSTEIN, SJ
    KASSIS, AI
    RADIATION RESEARCH, 1992, 129 (03) : 309 - 314
  • [45] TURNOVER OF I-125 LABELED HEMOPEXIN IN MAN
    KOSKELO, P
    KEKKI, M
    MUSTAJOKI, P
    VALMET, E
    ENZYME, 1974, 17 (1-2) : 116 - 121
  • [46] TURNOVER OF I-125 LABELED HEMOPEXIN IN MAN
    KOSKELO, P
    KEKKI, M
    MUSTAJOK.P
    SCANDINAVIAN JOURNAL OF CLINICAL & LABORATORY INVESTIGATION, 1973, 31 : 26 - 26
  • [47] AN OPTIMIZED METHOD FOR MEASURING CYCLOSPORINE-A WITH I-125 LABELED CYCLOSPORINE
    FELDER, RA
    MIFFLIN, TE
    BASTANI, B
    CLINICAL CHEMISTRY, 1986, 32 (07) : 1378 - 1382
  • [48] PRODUCTION AND APPLICATION OF I-123 LABELED M-IODOBENZYLGUANIDINE (I-123-METAIODOBENZYLGUANIDINE)
    WASHBURN, LC
    KHOSLA, RC
    WILLIAMS, CC
    GELFAND, MJ
    MAXON, HR
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1993, 206 : 90 - NUCL
  • [49] PREPARATION AND CHARACTERIZATION OF I-125 LABELED PROGESTERONE DERIVATIVES FOR THE DEVELOPMENT OF A RADIOIMMUNOASSAY FOR PROGESTERONE
    KOTHARI, K
    PILLAI, MRA
    JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY-ARTICLES, 1994, 177 (02): : 261 - 269
  • [50] RAPID METHOD FOR PREPARATION OF [I-125]ALPHA-BUNGAROTOXIN
    ELDEFRAWI, ME
    FERTUCK, HC
    ANALYTICAL BIOCHEMISTRY, 1974, 58 (01) : 63 - 70
12345