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. 1980 Aug 22;66(1):65-71.
doi: 10.1016/0014-2999(80)90295-2.

Modification of the proline residue of TRH enhances biological activity and inhibits degradation

D Brewster, P W Dettmar, A G Lynn, G Metcalf, B A Morgan, M J Rance

Modification of the proline residue of TRH enhances biological activity and inhibits degradation

D Brewster et al. Eur J Pharmacol. .

Abstract

An analogue of TRH with a modified proline residue (Pyr-His-MepNH2) has been synthesised and evaluated. In CNS, but not endocrine tests the analogue had improved activity compared to TRH and was more resistant to enzymatic degradation. A metabolite of TRH, His-Pro, was without biological activity. It is concluded that the biological actions attributed to TRH are due to the parent tripeptide rather than His-Pro and that these actions can be enhanced by improving the biological stability of TRH.

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