SINGLE DOSE LONG-TERM SUPPRESSION OF TESTOSTERONE SECRETION BY A GONADOTROPIN-RELEASING-HORMONE ANTAGONIST (ANTIDE) IN MALE MONKEYS

被引:19
作者
EDELSTEIN, MC [1 ]
GORDON, K [1 ]
WILLIAMS, RF [1 ]
DANFORTH, DR [1 ]
HODGEN, GD [1 ]
机构
[1] EASTERN VIRGINIA MED SCH,JONES INST REPROD MED,DEPT OBSTET & GYNECOL,NORFOLK,VA 23510
关键词
D O I
10.1016/0010-7824(90)90104-4
中图分类号
R71 [妇产科学];
学科分类号
100211 ;
摘要
This study was designed to find the minimal single dose of Antide (Nal-Lys GnRH antagonist) that would provide long-term inhibition of serum testosterone levels in adult male monkeys. At 3 mg/kg (sc), Antide blocked testosterone secretion for only a few days. However, when the dose of Antide was raised to 10 mg/kg, some of the males manifested testosterone inhibition lasting more than 60 days, while shorter durations of action were found in others. These preliminary findings increase our interest in studying Antide as a potential male contraceptive agent, when combined with androgen replacement therapy, as well as for therapeutic applications in men having prostatic carcinoma. Importantly, Antide lacks the sometimes deleterious "flare" effect known to occur when GnRH agonists are used to treat these patients. © 1990.
引用
收藏
页码:209 / 214
页数:6
相关论文
共 8 条
[1]   A COMPARISON OF THE SUPPRESSIVE EFFECTS OF TESTOSTERONE AND A POTENT NEW GONADOTROPIN-RELEASING HORMONE ANTAGONIST ON GONADOTROPIN AND INHIBIN LEVELS IN NORMAL MEN [J].
BAGATELL, CJ ;
MCLACHLAN, RI ;
DEKRETSER, DM ;
BURGER, HG ;
VALE, WW ;
RIVIER, JE ;
BREMNER, WJ .
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1989, 69 (01) :43-48
[2]   EXTENDED PRESENCE OF ANTIDE (NAL-LYS GNRH ANTAGONIST) IN CIRCULATION - PROLONGED DURATION OF GONADOTROPIN INHIBITION MAY DERIVE FROM ANTIDE BINDING TO SERUM-PROTEINS [J].
DANFORTH, DR ;
GORDON, K ;
LEAL, JA ;
WILLIAMS, RF ;
HODGEN, GD .
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1990, 70 (02) :554-556
[3]   PROLONGED DURATION OF GONADOTROPIN INHIBITION BY A 3RD GENERATION GNRH ANTAGONIST [J].
LEAL, JA ;
WILLIAMS, RF ;
DANFORTH, DR ;
GORDON, K ;
HODGEN, GD .
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1988, 67 (06) :1325-1327
[4]   PROBING STUDIES ON MULTIPLE DOSE EFFECTS OF ANTIDE (NAL-LYS) GNRH ANTAGONIST IN OVARIECTOMIZED MONKEYS [J].
LEAL, JA ;
GORDON, K ;
WILLIAMS, RF ;
DANFORTH, DR ;
ROH, SI ;
HODGEN, GD .
CONTRACEPTION, 1989, 40 (05) :623-633
[5]   DESIGN, SYNTHESIS AND BIOASSAYS OF ANTAGONISTS OF LHRH WHICH HAVE HIGH ANTIOVULATORY ACTIVITY AND RELEASE NEGLIGIBLE HISTAMINE [J].
LJUNGQVIST, A ;
FENG, DM ;
TANG, PFL ;
KUBOTA, M ;
OKAMOTO, T ;
ZHANG, YW ;
BOWERS, CY ;
FOLKERS, K .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 148 (02) :849-856
[6]  
MORTOLA JF, 1989, FERTIL STERIL, V51, P957
[7]   [AC-D-NAL(2)1,4FD-PHE2,D-TRP3,D-ARG6]-LHRH, A POTENT ANTAGONIST OF LHRH, PRODUCES TRANSIENT EDEMA AND BEHAVIORAL-CHANGES IN RATS [J].
SCHMIDT, F ;
SUNDARAM, K ;
THAU, RB ;
BARDIN, CW .
CONTRACEPTION, 1984, 29 (03) :283-289
[8]   SUSTAINED INHIBITION OF SPERM PRODUCTION AND INHIBIN SECRETION INDUCED BY A GONADOTROPIN-RELEASING HORMONE ANTAGONIST AND DELAYED TESTOSTERONE SUBSTITUTION IN NON-HUMAN PRIMATES (MACACA-FASCICULARIS) [J].
WEINBAUER, GF ;
KHURSHID, S ;
FINGSCHEIDT, U ;
NIESCHLAG, E .
JOURNAL OF ENDOCRINOLOGY, 1989, 123 (02) :303-310