PMID: 6987534Mar 27, 1980Paper

Luteinising hormone-releasing and anti-fertility properties of a glucagon-selective somatostatin analogue

F J BexE Lien


The hypothalamic tetradecapeptide, somatostatin (SRIF), inhibits the secretion of growth hormone (GH) and numerous other hormones, including insulin and glucagon. Attempts to use SRIF as an adjunct in the treatment of diabetes mellitus met with limited success due to its short biological half-life and the undesirable diabetogenic activity of its insulin-lowering properties. Efforts at synthesis have yielded SRIF derivatives with prolonged GH-lowering activity which did not suppress glucagon or had equivalent insulin-inhibiting activity as well as several short-acting compounds with the appropriate glucagon specificity. A dodecapeptide analogue [des-Ala, Gly] His-D-Trp-SRIF (Wy-41, 747) has been identified that combines selective inhibition of GH and glucagon release with prolonged activity. However, in routine pharmacological tests chronic treatment of mature rats with Wy-41, 747 produced anti-reproductive effects resembling those described for luteinising hormone (LH)-releasing hormone (RH) and its agonists. We report here that Wy-41, 747, unlike SRIF and other of its analogues tested, releases LH, induces ovulation and inhibits pregnancy when administered before or after implantation; these properties are traditionally associ...Continue Reading


Mar 1, 1979·International Journal of Gynaecology and Obstetrics : the Official Organ of the International Federation of Gynaecology and Obstetrics·A CorbinF Bex
Aug 22, 1977·Biochemical and Biophysical Research Communications·E LienJ P Yardley
Jul 1, 1978·Endocrinology·E Lien, V M Garsky
Jan 1, 1976·Annual Review of Medicine·R Guillemin, J E Gerich
Jan 24, 1977·Biochemical and Biophysical Research Communications·C MeyersF Labrie
May 1, 1977·The Journal of Clinical Endocrinology and Metabolism·W WaldhäuslE Deutsch
Nov 22, 1976·Biochemical and Biophysical Research Communications·D SarantakisR L Fenichel
Nov 1, 1976·Hormone and Metabolic Research = Hormon- Und Stoffwechselforschung = Hormones Et Métabolisme·P E Lins, S Efendić
Jul 22, 1975·Biochemical and Biophysical Research Communications·J RivierW Vale
Dec 8, 1973·Lancet·K G AlbertiH Orskov
Apr 1, 1973·Endocrinology·A BartkeB V Caldwell
Oct 1, 1973·The Journal of Clinical Endocrinology and Metabolism·T M SilerR Guillemin

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