ACTH (1-39) is a potent agonist of melanocortin receptor 2 (MC2R) with an EC50 value of 57 pM in HeLa cells expressing the mouse receptor.1 It induces accumulation of cAMP and release of corticosterone from rat adrenal cells in a concentration-dependent manner.2 ACTH (1-39) also protects neurons from death induced by staurosporine , glutamate, NMDA , AMPA , kainate, quinolinic acid , and reactive oxygen species when used at a concentration of 400 nM.3 Formulations containing ACTH (1-39) have been used in the treatment of systemic lupus erythematosus.
References
1. Kapas, S., Cammas, F.M., Hinson, J.P., et al. Agonist and receptor binding properties of adrenocorticotropin peptides using the cloned mouse adrenocorticotropin receptor expressed in a stably transfected HeLa cell line. Endocrinology 137(8), 3291-3294 (1996).
2. Bristow, A.F., Gleed, C., FauchÈre, J.L., et al. Effects of ACTH (corticotropin) analogues on steroidogenesis and cyclic AMP in rat adrenocortical cells. Evidence for two different steroidogenically responsive receptors. Biochem J. 186(2), 599-603 (1980).
3. Lisak, R.P., Nedelkoska, L., Bealmear, B., et al. Melanocortin receptor agonist ACTH 1-39 protects rat forebrain neurons from apoptotic, excitotoxic and inflammation-related damage. Exp. Neurol. 273, 161-167 (2015).