Comparison of structural requirements of alpha-MSH and ACTH for inducing excessive grooming and pigment dispersion |
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Authors: | B M Spruijt P N De Graan A N Eberle W H Gispen |
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Institution: | 1. Division of Molecular Neurobiology Institute of Molecular Biology State University of Utrecht, Padualaan 8, 3584 CH Utrecht, The Netherlands;2. Rudolf Magnus Institute for Pharmacology State University of Utrecht, Padualaan 8, 3584 CH Utrecht, The Netherlands;1. Laboratory of Endocrinology, Department of Research University Hospital and University Children''s Hospital, CH-4031 Basel, Switzerland |
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Abstract: | alpha-MSH and ACTH-like peptides are known to play an important role in the adaptation of many vertebrates to a new environment. These peptides induce pigment dispersion in amphibian melanophores through a receptor-mediated mechanism. In this study we compared the structural requirements of these peptides for melanotropic activity on Xenopus laevis melanophores with those for inducing excessive grooming in the rat. With the exception of ACTH1-24 there is a close resemblance in structure-activity relationships of the fragments and analogs tested in the two bioassays. Nle4,-D-Phe7]-alpha-MSH is extremely active in both assays. Weak agonists such as Leu9]-alpha-MSH did not possess antagonistic properties either in the melanophore assay or in the excessive grooming test. The data suggest that the mechanism of action of alpha-MSH-like peptides in rat brain is receptor-mediated like their action on melanophores. |
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Keywords: | α-MSH receptors Melanotropins Pigment dispersion Excessive grooming Structure-activity |
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