Abstract
Behavioural activities of peptides related to corticotrophin and lipotrophin were studied in active and passive avoidance tests in rats. When searching for an active core in the ACTH-molecule which would be responsible for activity in the pole-jumping test, we found that essential information for this type of activity was not confined to the minimal fragment 4–7, but was also present in the sequences 7–10, Ac-(11–13)-NH2 and 25–39, indicating a redundance of information. Through the introduction of certain modifications in the sequence ACTH4–10, selectivity of action could be improved and the potency increased a thousandfold. Another increase in potency by a factor of at least 1000 could be obtained by C-terminal elongation with a modified ACTH11–16 sequence. The finding that [Met5] enkephalin was equally as active as ACTH4–10 in the pole-jumping test was used as an additional argument for the suggestion that the latter peptide assumes an α-helix conformation at the receptor site. When fragments of β-endorphin were tested for their capacity to inhibit extinction of a conditioned avoidance response in the pole-jumping test, the sequence 62–76 appeared to be the most active one, whereas in the series of peptides related to γ-endorphin which accelerate extinction, the fragment 66–77 appeared to be the shortest one to give a significant response. The possible function of peptides related to corticotrophin and lipotrophin in situations of stress or in psychotic disorders is discussed.
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Greven, H.M., de Wied, D. (1980). Structure and behavioural activity of peptides related to corticotrophin and lipotrophin. In: Hormones and the Brain. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-8709-8_10
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DOI: https://doi.org/10.1007/978-94-009-8709-8_10
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