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A series of synthetic human TRH analogues was tested for thyroid stimulating and thyrotropic activities in the rat in order to determine the contribution of the second amino group of the TRH molecule to the bioactivity of the neuropeptide. The analogue with the lowest TSH-stimulating activity, A[delta Pro]TRH, was found to be a poor TSH stimulator. The presence of an amino group at position 2 of the TRH molecule, as a prerequisite for the TSH-stimulating activity, could also be excluded from the point of view of the peptide structure. A major limitation of the studies was the TSH-stimulating activity of A[delta Pro]TRH, the analog of the TRH molecule which is 100% homologous to TRH and was found to be the most potent TRH agonist in our previous study. In order to avoid this problem we used a series of TRH analogues with an unmodified TRH molecule. We found the most potent TRH analogue to be A[delta Pro]TRH-Ile, which was 1000-fold less active than A[delta Pro]TRH, the TRH molecule, in the TSH-stimulating test. Furthermore, this analogue was found to be the most potent thyrotropic stimulator. The thyrotropic activity of A[delta Pro]TRH-Ile was more than 100-fold higher than that of TRH-Ile, which was a comparable thy 0b46394aab
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