- Synthesis of Thyrotropin-Releasing Hormone Analogues. 1. Complete Dissociation of Central Nervous Effects from Thyrotropin-Releasing Activity
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Twenty-four thyrotropin-releasing hormone (TRH) analogues containing mainly aliphatic amino acids in position 2 were synthesized and tested for central nervous system (CNS) and hormonal (TSH) activity.Application of the pentafluorophenyl ester method in t
- Szirtes, Tamas,Kisfaludy, Lajos,Palosi, Eva,Szporny, Laszlo
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p. 741 - 745
(2007/10/02)
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- Potential thyroliberin affinity labels. II: Chloroacetyl substituted phenylalanyl prolineamides
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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.
- Goebel,Currie,Bowers
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p. 1062 - 1064
(2007/10/02)
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