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. 1978 Mar;302(1):31-6.
doi: 10.1007/BF00586593.

ACTH-induced lipolysis in rat adipocytes: structure-activity relationships

F A Opmeer, J M van Ree, D de Wied

ACTH-induced lipolysis in rat adipocytes: structure-activity relationships

F A Opmeer et al. Naunyn Schmiedebergs Arch Pharmacol. 1978 Mar.

Abstract

The lipolytic action of natural porcine ACTH1(-39) and of a number of highly purified synthetic ACTH peptide fragments was studied using rat adipocytes. Of the analogues tested, only ACTH1(-24) exhibited full lipolytic activity with respect to intrinsic activity and affinity. Several shorter fragments appeared to be full agonists but had lower affinity. Fragments ACTH5(-10) and ACTH7(-10) were inactive. No antagonistic effects against the lipolytic action of ACTH could be demonstrated with substimulatory doses of ACTH1(-16), ACTH1(-10), ACTH7(-24) and ACTH11(-24). Based on the relative potency derived from dose-response curves, a more refined model with respect to the active centers being encoded in various sequences of the hormone, is proposed.

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