ISSN:
1573-3904
Keywords:
Anxiety
;
Attention memory
;
CCK-B agonists
;
CCK-B receptor subsites
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Since the biochemical and pharmacological profile of BC 197 and BC 264,two CCK8-derived agonists with high specificity for CCK-Breceptors, suggests their potential interaction with two CCK-B receptorsubsites, it appeared essential to design new series of compounds that wouldbe able to discriminate between these two subsites. As CCK4 isthe shortest fragment of CCK which interacts selectively with CCK-Breceptors, compounds derived from the C-terminal tetrapeptide domain of BC264, Boc-Trp-(NMe)Nle-Asp-Phe-NH2, and of the cyclic compoundBC 197, were prepared. While RB 360(N-(cycloamido)-α-Me(R)Trp-[(2S)-2-amino-9-((cycloamido)carbonyl)nonanoyl]-Asp-Phe-NH2), like BC 197, has a CCK-B1 profilewith anxiogenic-like effects in the elevated plus-maze test, RB 400(HOOC-CH2-CO-Trp-(NMe)Nle-Asp-Phe-NH2), like BC264, seems to be a specific CCK-B2 agonist, able to increaseattention and/or memory processes in the Y-maze test.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1008890031134
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