Antiamnesic properties of analogs and mimetics of the tripeptide human urocortin 3.
Amino Acids
; 48(9): 2261-6, 2016 09.
Article
in En
| MEDLINE
| ID: mdl-27262310
ABSTRACT
Amnesia is a deficit in memory caused by brain damage, disease, or trauma. Until now, there are no successful medications on the drug market available to treat amnesia. Short analogs and mimetics of human urocortin 3 (Ucn 3) tripeptide were synthetized and tested for their action against amnesia induced by eletroconvulsion in mice. Among the 16 investigated derivatives of Ucn 3 tripeptide, eight compounds displayed antiamnesic effect. Our results proved that the configuration of chiral center of glutamine does not affect the antiamnesic properties. Alkyl amide or isoleucyl amide at the C-terminus may lead to antiamnesic compounds. As concerned the N-terminus, acetyl, Boc, and alkyl ureido moieties were found among the active analogs, but the free amino function at the N-terminus usually led to an inactive derivatives. These observations may lead to the design and synthesis of small peptidomimetics and amino acid derivatives as antiamnesic drug candidates, although the elucidation of the mechanism of the action requires further investigations.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oligopeptides
/
Corticotropin-Releasing Hormone
/
Urocortins
/
Peptidomimetics
/
Amnesia
Limits:
Animals
/
Female
/
Humans
Language:
En
Journal:
Amino Acids
Journal subject:
BIOQUIMICA
Year:
2016
Document type:
Article
Affiliation country:
Hungary
Publication country:
AT
/
AUSTRIA
/
ÁUSTRIA