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Synthesis of some structural analogues of LH-RH modified in position 5, their in vivo and in vitro gonadotropin-releasing activity and immunoreactivity
Authors:H Künzi  D Gillessen  A Trzeciak  R O Studer  B Kerdelhué  M Jutisz  W Lotz
Abstract:Four analogues of LH-RH modified in position 5 have been synthesized using either classical procedures or the solid phase method. The gonadotropin-releasing activities were determined by radioimmunological measurements of LH and FSH in vivo and in vitro and the immunoreactivities by a specific LH-RH radioimmunoassay (RIA). The following relative potencies and immunoractivities were found:
in vivo in vitro Immuno-reactivity
LH-RH: 100 % 100 % 100 %
Tyr(Me)5] -LH-RH: 8.6% 6.0% 40.0%
Phe5] -LH-RH: 42.5% 27.5% 17.0%
Cha5]
  • a Abbreviations were used according to 37]; Cha = cyclohexyl-L-alanine.
  • -LH-RH: 22.4% 27.8% 10.0%
    Gly5] -LH-RH: 0.1% 0.5% 0.7%

    Citing Literature

    Volume 57 , Issue 7 6 November 1974

    Pages 2131-2139

    Keywords:
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