European Journal of Medicinal Chemistry p. 47 - 61 (1993)
Update date:2022-08-04
Topics:
Boden, P. R.
Eden, J. M.
Higginbottom, M.
Hill, D. R.
Horwell, D. C.
et al.
This paper outlines the synthesis and C-terminal structure-activity relationships (SAR) of a series of α-methyl tryptophanylphenethylamide analogues of the neuropeptide cholecystokinin (CCK).CCK-B and CCK-A receptor binding affinities of these analogues are described and the contributions of the various side chains on the phenethylamide moiety to binding affinity are discussed.Several of the compounds prepared have CCK-B receptor binding affinities similar to that found with the endogenous neuropeptide CCK-26-33 (sulphated) (CCK-B, IC50 = 0.3 nM) and are highly selective over the CCK-A receptor.Amongst the most potent of the compounds synthesized are
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