Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors.
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.
Mutulis
Felikss
F
Department of Pharmaceutical Biosciences, Division of Pharmacology, Uppsala Biomedical Center, PO Box 591, Uppsala University, S-751 24 Uppsala, Sweden.
Mutule
Ilze
I
Lapins
Maris
M
Wikberg
Jarl E S
JE
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
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