[Synthesis of thyreoliberin (TRF)].
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Biomedical subjects
Publications and source records attributed to H Niedrich.
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Under the condition of receptor blockade produced by continuous presence of an agonist in the organ bath, it was attempted to determine the dissociation constants for C-terminal partial sequences of the substance P at an isolated guinea pig ileum, by analogy with the method involving irreversible antagonists, and to compare them with the biological activity at the guinea pig ileum and the rat colon (ED50 values). Differentiation of the biological activity at the guinea pig ileum into affinity and "intrinsic efficacy" allows one to explain quantitative differences in determining the biological value on both isolated organs, and to reveal the contribution of the individual amino acids to affinity and "intrinsic efficacy".
C-terminal pentapeptides of eledoisin, physalaemin, and the substance P, when N-substituted with acetyl, halogenacetyl and other acyl residues, are increased in their action more than 100fold, reaching the activity of acylated hexa- and heptapeptides. The effect found with a number of compounds is interpreted as the influence of predominantly hydrophobic substituents upon the peptide sequence essential for the action. Polar groups in the acylic residue seem to cause additional increase in action.
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