Spruijt B M, De Graan P N, Eberle A N, Gispen W H
Peptides. 1985 Nov-Dec;6(6):1185-9. doi: 10.1016/0196-9781(85)90448-6.
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.
已知α-促黑素（alpha-MSH）和促肾上腺皮质激素（ACTH）样肽在许多脊椎动物适应新环境中发挥重要作用。这些肽通过受体介导的机制诱导两栖动物黑素细胞中的色素分散。在本研究中，我们比较了这些肽对非洲爪蟾黑素细胞的促黑素活性与对大鼠诱导过度梳理行为的结构要求。除了促肾上腺皮质激素1-24（ACTH1-24）外，在两种生物测定中测试的片段和类似物的构效关系非常相似。[Nle4，-D-Phe7]-α-促黑素在两种测定中都极具活性。弱激动剂如[Leu9]-α-促黑素在黑素细胞测定或过度梳理试验中均不具有拮抗特性。数据表明，α-MSH样肽在大鼠脑中的作用机制与其对黑素细胞的作用一样是受体介导的。
