Biological activity of TRH thionalogue and its diastereoisomers
Alexandrová, M.; Strbák, V.; Herman, Z.S.; Stachura, Z.; Kruszyński, M.
Endocrinologia Experimentalis 21(1): 43-49
1987
ISSN/ISBN: 0013-7200 PMID: 3106009 Document Number: 287183
Binding affinity and TSH-releasing activity of [Prot3] TRH analogue (L-pyroglutamyl-L-histidyl-L-proline thioamide), TRH and their LDL and LLD diastereoisomers were compared in rats. Binding affinity and dose-related increase of TSH secretion were similar for both [Prot3] TRH and TRH. Moreover, similar effect of both peptides on sleeping time and motoric activity of rat was found. Substitution of L- for D-amino acids of TRH and [Prot3] TRH decreased the binding affinity and TSH-releasing activity as well. It was concluded that [Prot3] TRH analogue is as active as native TRH.