Potential thyroliberin affinity labels II: Chloroacetyl substituted phenylalanyl prolineamides.
Three analogs of thyroliberin (I) were prepared. These compounds, N-m-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIa), N-p-chloroacetylbenzoyl-phenylalanyl-prolineamide (VIb) and N-chloroacetyl-alanyl-phenylalanyl-prolineamide (IX), were designed as potential I antagonist affinity labels. However, no significant antagonist activity was observed. Compounds VIa and IX were found to have weak agonist activity. Cyclo (Phe-Pro) an analog of the I metabolite, cyclo (His-Pro), was found, however, to have significant I antagonist activity, but no agonist activity.
D000345:Affinity Labels / Q000138:chemical synthesis*; D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D051381:Rats; D013329:Structure-Activity Relationship; D013973:Thyrotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000032:analysis* / Q000138:chemical synthesis
D000345:Affinity Labels; D013973:Thyrotropin-Releasing Hormone