PMID- 25288495 OWN - NLM STAT- MEDLINE DCOM- 20150722 LR - 20220409 IS - 1464-3391 (Electronic) IS - 0968-0896 (Print) IS - 0968-0896 (Linking) VI - 22 IP - 21 DP - 2014 Nov 1 TI - Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors. PG - 5831-7 LID - S0968-0896(14)00671-3 [pii] LID - 10.1016/j.bmc.2014.09.025 [doi] AB - A series of Arg-Phe-NH2 peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models. CI - Copyright (c) 2014 Elsevier Ltd. All rights reserved. FAU - Hin, Niyada AU - Hin N AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Alt, Jesse AU - Alt J AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Zimmermann, Sarah C AU - Zimmermann SC AD - Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Delahanty, Greg AU - Delahanty G AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Ferraris, Dana V AU - Ferraris DV AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Rojas, Camilo AU - Rojas C AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Li, Fengxian AU - Li F AD - Center for the Study of Itch and Departments of Anesthesiology and Anatomy & Neurobiology, Washington University School of Medicine, St Louis, MO 63110, United States. FAU - Liu, Qin AU - Liu Q AD - Center for the Study of Itch and Departments of Anesthesiology and Anatomy & Neurobiology, Washington University School of Medicine, St Louis, MO 63110, United States. FAU - Dong, Xinzhong AU - Dong X AD - The Solomon H. Snyder Department of Neuroscience, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Slusher, Barbara S AU - Slusher BS AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States; Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States. FAU - Tsukamoto, Takashi AU - Tsukamoto T AD - Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States; Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States. Electronic address: ttsukamoto@jhmi.edu. LA - eng GR - R01 NS054791/NS/NINDS NIH HHS/United States GR - 2R01NS054791/NS/NINDS NIH HHS/United States PT - Journal Article PT - Research Support, N.I.H., Extramural PT - Research Support, Non-U.S. Gov't DEP - 20140919 PL - England TA - Bioorg Med Chem JT - Bioorganic & medicinal chemistry JID - 9413298 RN - 0 (MrgC11 protein, mouse) RN - 0 (Mrgprc protein, rat) RN - 0 (Neuropeptides) RN - 0 (Peptidomimetics) RN - 0 (Receptors, G-Protein-Coupled) RN - 0 (Small Molecule Libraries) RN - 0 (mas-related gene-X1 receptor, human) RN - 34388-59-5 (arginylphenylalaninamide) SB - IM MH - Animals MH - HEK293 Cells MH - Humans MH - Mice MH - Neuropeptides/chemical synthesis/*chemistry/metabolism MH - Peptidomimetics/pharmacology MH - Protein Binding/drug effects MH - Rats MH - Receptors, G-Protein-Coupled/*agonists/genetics/metabolism MH - Small Molecule Libraries/chemical synthesis/chemistry/metabolism/pharmacology MH - Transfection PMC - PMC4254045 MID - NIHMS629545 OTO - NOTNLM OT - Agonist OT - Arginine mimetic OT - Mas-related gene (Mrg) receptors OT - Peptidomimetic EDAT- 2014/10/08 06:00 MHDA- 2015/07/23 06:00 PMCR- 2015/11/01 CRDT- 2014/10/08 06:00 PHST- 2014/07/27 00:00 [received] PHST- 2014/09/05 00:00 [revised] PHST- 2014/09/11 00:00 [accepted] PHST- 2014/10/08 06:00 [entrez] PHST- 2014/10/08 06:00 [pubmed] PHST- 2015/07/23 06:00 [medline] PHST- 2015/11/01 00:00 [pmc-release] AID - S0968-0896(14)00671-3 [pii] AID - 10.1016/j.bmc.2014.09.025 [doi] PST - ppublish SO - Bioorg Med Chem. 2014 Nov 1;22(21):5831-7. doi: 10.1016/j.bmc.2014.09.025. Epub 2014 Sep 19.