Treatment of experimental DMBA induced mammary carcinoma with Cetrorelix (SB-75): a potent antagonist of luteinizing hormone-releasing hormone

1992 ◽  
Vol 118 (1) ◽  
pp. 44-49 ◽  
Author(s):  
Thomas Reissmann ◽  
Peter Hilgard ◽  
Johannes H. Harleman ◽  
J�rgen Engel ◽  
Ana M. Comaru-Schally ◽  
...  
Keyword(s):  
Luteinizing Hormone ◽  
Mammary Carcinoma ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Potent Antagonist

Antagonists of LHRH with Histidine in the Priority Position 8

1993 ◽  
Vol 48 (6) ◽  
pp. 812-816 ◽  
Author(s):  
Anna Janecka ◽  
Si-Mei Shan ◽  
Cyril Bowers ◽  
Karl Folkers
Keyword(s):  
Luteinizing Hormone ◽  
Histamine Release ◽  
Side Effect ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Significant Release ◽  
Potent Antagonist ◽  
Antiovulatory Activity

Sixteen new designs of antagonists of the luteinizing hormone releasing hormone (LHRH) with histidine in position 8 were synthesized, because this position is critical both for antiovulatory activity and the side effect of histamine release. The most potent antagonist was NAcDQal-DpClPhe–D 3 Pal– Ser–cPzACAla–DPicLys– Leu– His – Pro –DAlaNH2, which showed 33% AOA at 0.25 μg. The histamine release was remarkably negligible by an ED50 of 308 μg/ml which is superior to 186 μg/ml for LHRH and comparable to 300 for Antide.The relative basicities of His, Arg, and ILys in position 8 of antagonists appear to influence both the level of potency of AOA and a negligible to a significant release of histamine. The least basic His8-analogs can have the lowest AOA and the highest ED50. The very basic Arg8-analogs can have the highest AOA and the lowest ED50. The moderately basic ILys8-analogs can be a compromise for acceptable levels of potency and safety.

Effect of luteinizing hormone-releasing hormone analogs containing cytotoxic radicals on growth of estrogen-independent MXT mouse mammary carcinoma in vivo

1992 ◽  
Vol 3 (2) ◽  
pp. 109-116 ◽  
Author(s):  
Karoly Szepeshazi ◽  
Andrew V Schally ◽  
Attila Juhasz ◽  
Attila Nagy ◽  
Tamas Janaky
Keyword(s):  
Luteinizing Hormone ◽  
Mammary Carcinoma ◽  
Mouse Mammary Carcinoma ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Hormone Analogs

Analogs of the Luteinizing Hormone Releasing Hormone having the Azagly10 Moiety with Antiovulatory Activity

1984 ◽  
Vol 39 (4) ◽  
pp. 528-532 ◽  
Author(s):  
Karl Folkers ◽  
Cyril Y. Bowers ◽  
Janusz Stepinski ◽  
Tomasz Plucinski ◽  
Masanori Sakagami ◽  
...  
Keyword(s):  
Luteinizing Hormone ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Potent Antagonist ◽  
Antiovulatory Activity

Twenty-four new analogs of the luteinizing hormone releasing hormone (LHRH) were synthesized and bioassayed for antiovulatory activity in rats. [N-Ac-3⊿Pro1, pF-D-Phe2, D-Trp3,6, Azagly10]-LHRH com pletely inhibited ovulation at 6 μg and was the most potent of the 24, and is a relatively potent antagonist in the field. The Azagly- and Ac-NHNH- and D-Alamoieties in position 10, and D-Arg in position 6, and diverse substitutions in position 1 were emphasized. D-Arg6 was inferior to D-Trp6, and pCl-D-Phe6 appeared superior to D-Trp6. D-Trp3,6 was superior to D-2-Nal3,6 and D-His3,6.

scholarly journals Postmenopause-Like Bone Loss by Mammary Carcinoma Walker256/S Which Secretes Luteinizing Hormone-Releasing Hormone

1999 ◽  
Vol 80 (2) ◽  
pp. 119-126 ◽  
Author(s):  
Yoshihiro Waki ◽  
Ken-ichi Miyamoto ◽  
Shinya Yamamoto ◽  
Yukie Saitoh ◽  
Shohei Kasugai ◽  
...  
Keyword(s):  
Luteinizing Hormone ◽  
Bone Loss ◽  
Mammary Carcinoma ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone
Sign in / Sign up

Export Citation Format

Share Document