Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.
Conformationally constrained dipeptoid analogues containing the type II' beta-turn mimic (2S,5s,11bR)-2-amino-3-oxohexahydroindolizino[8,7-b]indole-5 -carboxylate framework in place of the alpha-MeTrp residue, show high binding affinity and selectivity for CCK-A receptors, suggesting that a turn-like conformation could contribute to the bioactive conformation at this CCK receptor subtype.
de la Figuera
N
N
Instituto de Química Médica (CSIC), Madrid, Spain.
Martín-Martínez
M
M
Herranz
R
R
García-López
M T
MT
Latorre
M
M
Cenarruzabeitia
E
E
del Río
J
J
González-Muñiz
R
R
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D007211:Indoles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D007212:Indolizines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D018716:Molecular Mimicry; D015394:Molecular Structure; D010179:Pancreas / Q000378:metabolism; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D012844:Sincalide / Q000378:metabolism