| Autor: |
Kalindjian SB; James Black Foundation, London, U.K., Buck IM, Cushnir JR, Dunstone DJ, Hudson ML, Low CM, McDonald IM, Pether MJ, Steel KI, Tozer MJ |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 1995 Oct 13; Vol. 38 (21), pp. 4294-302. |
| DOI: |
10.1021/jm00021a019 |
| Abstrakt: |
We have recently described a novel series of nonpeptidic cholecystokinin-B (CCKB)/gastrin receptor antagonists based on a dibenzobicyclo[2.2.2]octane skeleton. We wish now to report on compounds arising out of our earlier work which have substantially greater affinity as antagonists for the CCKB/gastrin receptor system and which maintain, or improve on, the already high selectivity with respect to CCKA receptors. Thus, cis-7-[[[(1S)-[[3,5-dicarboxy-phenyl)amino]carbonyl]-2- phenylethyl]amino]carbonyl]-8-[[(1-adamantylmethyl)amino]- carbonyl]-2,3:5,6-dibenzobicyclo[2.2.2]octane expressed a pKi of 8.80 in mouse cortical membranes at CCKB/gastrin receptors. The selectivity for these receptors over CCKA receptors was in the order of 1000-fold. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
