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New, highly active antagonists of LHRH with acylated lysine and p-aminophenylalanine in positions 5 and 6

Content Provider	Scilit
Author	Janecka, Anna Janecki, Tomasz Bowers, Cyril Y. Folkers, Karl
Copyright Year	2009
Description	Journal: International journal of peptide and protein research A series of antagonists of the luteinizing hormone releasing hormone (LHRH) with substitutions in position 5 and/or 6 that included acylated lysine or p-aminophenylalanine were synthesized, characterized and tested for antiovulatory activity (AOA) in rats, and histamine releasing activity. Some of these antagonists were considerably more soluble at neutral pH than antagonists like Antide. Of 37 new antagonists, the best physico-chemical and biological properties were found for the following two analogs: NAcDNal-DCpa-DPal-Ser-PicLys-D(PicSar)Lys- Leu-ILys-Pro-DAlaNH2 (named Sartide) and NAcDNal-DCpa-DPal-Ser-Tyr-D(PicSar)Lys-Leu-IL ys-Pro-DAlaNH2. They are both soluble in water, inhibit ovulation completely at 0.5 microgram per rat, and have ED50 values for histamine release of about 30 micrograms/mL.
Related Links	http://onlinelibrary.wiley.com/doi/10.1111/j.1399-3011.1994.tb00399.x/pdf
Ending Page	23
Page Count	5
Starting Page	19
ISSN	03678377
DOI	10.1111/j.1399-3011.1994.tb00399.x
Journal	International journal of peptide and protein research
Issue Number	1
Volume Number	44
Language	English
Publisher	Wiley-Blackwell
Publisher Date	2009-01-12
Access Restriction	Open
Subject Keyword	Journal: International journal of peptide and protein research Medicinal Chemistry Antiovulatory Activity Histamine Release Luteinizing Hormone Releasing Hormone Solid‐phase Peptide Synthesis
Content Type	Text
Resource Type	Article
Subject	Biochemistry

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