Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist.

ABSTRACT:

Background

The activation of melanocortin 1 receptor (MC1R) on melanocytes stimulates the production of eumelanin. A tridecapeptide α melanocyte-stimulating hormone (αMSH) is known to induce skin pigmentation.

Objectives

We characterised the properties of a novel oral MC1R agonist dersimelagon (MT-7117) with respect to its specific binding to MC1R, downstream signalling and eumelanin production in experimental models.

Methods

The competitive binding and production of intracellular cyclic adenosine 3', 5'-monophosphate in cells expressing recombinant melanocortin receptors were examined. A mouse melanoma cell line B16F1 was used for the evaluation of in vitro melanin production. The in vitro activity of MT-7117 was determined with αMSH and [Nle⁴, D-Phe⁷

SUBMITTER: Suzuki T 

PROVIDER: S-EPMC9060023 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature