title: Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.
abstract: Presumed pharmacophoric groups of melanocortin peptides (naphthalene, amino or guanidine, and indole moieties) were combined in mimetics molecules looking for their favorable location for activity at melanocortin (MC) receptors. Twenty-two compounds were prepared and tested. The best of these displayed micromolar affinities for the MC receptors.
authors.affiliation: Department of Pharmaceutical Biosciences, Division of Pharmacology, Uppsala Biomedical Center, PO Box 591, Uppsala University, S-751 24 Uppsala, Sweden.
authors.forename: Felikss
authors.initials: F
authors.lastname: Mutulis
authors.forename: Ilze
authors.initials: I
authors.lastname: Mutule
authors.forename: Maris
authors.initials: M
authors.lastname: Lapins
authors.forename: Jarl E S
authors.initials: JE
authors.lastname: Wikberg
mesh_terms: D000586:Amination; D001667:Binding, Competitive; D002460:Cell Line; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008956:Models, Chemical; D015394:Molecular Structure; D009281:Naphthalenes / Q000737:chemistry / Q000378:metabolism*; D010084:Oxidation-Reduction; D010455:Peptides / Q000138:chemical synthesis; D011485:Protein Binding; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D018043:Receptors, Corticotropin / Q000819:agonists / Q000378:metabolism*; D044101:Receptors, Melanocortin
chemical_list: D007211:Indoles; D007457:Iodine Radioisotopes; D009281:Naphthalenes; D010455:Peptides; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D018043:Receptors, Corticotropin; D044101:Receptors, Melanocortin; C086971:melanocortin 5 receptor; C031721:naphthalene; C030374:indole