Conformationally constrained alpha-melanotropin analogs with specific central nervous system activity

Abstract

Abstract Novel compounds which are analogs of alpha -melanotropin and which exhibit reactivity for the central nervous system receptors without exhibiting substantial reactivity for the peripheral receptors are disclosed. The compounds of the present invention are polypeptides of the formula: <IMAGE> wherein R1 is a substituted or unsubstituted aromatic radical; R2 is hydrogen or a methyl group; R3 is carboxylate, carboxamide, hydroxymethyl, or aldehyde group or a peptide residue; R4 is a simple amino acid residue; R5 is a simple amino acid residue; R6 and R7, which may be the same or different, are hydrogen, methyl or lower alkyl having one to five carbon atoms; R8 and R9, which may be the same or different, are hydrogen, methyl or lower alkyl having one to five carbon atoms; X and Y are sulfur, methylene, SO, or SO2; Z is -NH2, <IMAGE> and n is an integer greater than or equal to 2. The noval compounds may be used in humans and lower animals to facilitate memory and behavior, improve fetal growth and development, enhance attention, improve socialization, stimulate sexual activity, reverse morphine analgesia, act as an antidepressant, act as an antipyretic and centrally direct effects on visceral functions.

Inventors

• 👤 Victor J. Hruby

Bibliographic Details