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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

✍ Scribed by Hans Künzi; Dieter Gillessen; Arnold Trzeciak; Rolf O. Studer; Bernard Kerdelhué; Marian Jutisz; Wolfgang Lotz

Publisher
John Wiley and Sons
Year
1974
Tongue
German
Weight
670 KB
Volume
57
Category
Article
ISSN
0018-019X

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✦ Synopsis

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%
[Phe^5^] ‐LH‐RH: 42.5% 27.5% 17.0%
[Cha^5^]Abbreviations were used according to [37]; Cha = cyclohexyl‐L‐alanine. ‐LH‐RH: 22.4% 27.8% 10.0%
[Gly^5^] ‐LH‐RH: 0.1% 0.5% 0.7%

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