Modified di- and tripeptides of the C-terminal portion of oxytocin and vasopressin as possible cognition activation agents

A number of peptides and modified peptides were synthesized and studied for their ability to reverse electroconvulsive shock-induced amnesia in rodents. A few of these peptides were selected for secondary evaluation in tests of short-term memory in rats and aged rhesus monkeys. A number of the pepti...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1986-06, Vol.29 (6), p.959-971
Main Authors: Nicolaides, E. D, Tinney, F. J, Kaltenbronn, J. S, Repine, J. T, DeJohn, D. A, Lunney, E. A, Roark, W. H
Format: Article
Language:English
Subjects:
Animals
Chemistry
Cognition - drug effects
Exact sciences and technology
Macaca mulatta
Memory, Short-Term - drug effects
Organic chemistry
Oxytocin - pharmacology
Peptides
Peptides - chemical synthesis
Peptides - pharmacology
Preparations and properties
Rats
Structure-Activity Relationship
Vasopressins - pharmacology
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Summary:A number of peptides and modified peptides were synthesized and studied for their ability to reverse electroconvulsive shock-induced amnesia in rodents. A few of these peptides were selected for secondary evaluation in tests of short-term memory in rats and aged rhesus monkeys. A number of the peptides and modified peptides were active in the amnesia reversal test. In selected secondary tests, however, the chosen compounds failed to show significant activity in enhancing memory. New methods for preparing methyleneamino and methyleneoxy isosteres of peptides are reported. Other modified peptides also included methylenethio, methylenesulfonyl, and ethylene isosteres in place of the normal peptide amide bond.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00156a012