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Increased potency of antagonists of the luteinizing hormone releasing hormone which have D-3-Pal in position 6
- Source :
- Biochemical and Biophysical Research Communications. 137:709-715
- Publication Year :
- 1986
- Publisher :
- Elsevier BV, 1986.
-
Abstract
- Ever increasing potency is an international goal for antagonists of the luteinizing hormone releasing hormone (LHRH). [N-Ac-D-2-Nal1,D-pClPhe2,D-3-Pal3,Ser4,Arg5,D-3-Pal6,Leu7,Arg8,Pro9,D-Ala10]-NH2 caused 60%/125 ng inhibition of ovulation in the rat, and appears to be the most potent antagonist yet described. Strategy of design was the replacement of D-Arg6 with D-3-Pal6 and of Tyr5 with Arg5. replacing Arg5 with His5 reduced activity by 50% at 250 ng. Both the Arg5 and His5 analogs showed 100% inihibition of ovulation at 0.5 μg. Of ten pairs of analogs with D-3-Pal6 and D-Arg6, 3 10 with D-3-Pal6 were more potent than those with D-Arg6. Histamine release was less for the D-3-Pal6 peptides of three pairs.
- Subjects :
- Male
Ovulation
medicine.medical_specialty
media_common.quotation_subject
Biophysics
In Vitro Techniques
Arginine
Histamine Release
Biochemistry
Gonadotropin-Releasing Hormone
Structure-Activity Relationship
chemistry.chemical_compound
Thyrotropin-releasing hormone receptor
Internal medicine
medicine
Animals
Potency
Amino Acids
Molecular Biology
media_common
Alanine
Antagonist
Rats, Inbred Strains
Cell Biology
Rats
Endocrinology
chemistry
Female
Luteinizing hormone
Histamine
Hormone
Subjects
Details
- ISSN :
- 0006291X
- Volume :
- 137
- Database :
- OpenAIRE
- Journal :
- Biochemical and Biophysical Research Communications
- Accession number :
- edsair.doi.dedup.....5e1523a1b280451eb6cb4e09ebd3ee07