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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
Author(s) -
Künzi Hans,
Gillessen Dieter,
Trzeciak Arnold,
Studer Rolf O.,
Kerdelhué Bernard,
Jutisz Marian,
Lotz Wolfgang
Publication year - 1974
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19740570728
Subject(s) - chemistry , in vivo , radioimmunoassay , in vitro , gonadotropin , endocrinology , stereochemistry , medicine , biochemistry , hormone , microbiology and biotechnology , biology
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: Textin vivo in vitro Immuno‐reactivityLH‐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%