- CCK2 receptor antagonists containing the conformationally constrained phenylalanine derivatives, including the new amino acid Xic
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The conformationally constrained analogues of phenylalanine, tetrahydroisoquinoline-3-carboxylic acid (Tic), Sic, Hic and Nic, and the new amino acid Xic have been incorporated into a potent and highly selective cholecystokinin-2 (CCK2) receptor antagonist (2) in place of the phenylalanine residue, producing compounds 15a-e. High selectivities for CCK2 over CCK1 were observed for compounds 15a-e. The in vitro profile of the analogue containing the Nic residue (15d) was identical to that of compound 2, whereas the alternative conformational constraints resulted in a significant loss of affinity. The apparent advantage of Nic in the context of these CCK2 ligands was subsequently demonstrated to be statistically significant.
- Gibson, Susan E,Guillo, Nathalie,Jones, Jerome O,Buck, Ildiko M,Kalindjian, S.Barret,Roberts, Sonia,Tozer, Matthew J
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p. 379 - 389
(2007/10/03)
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- Incorporation of conformationally constrained phenylalanine derivatives TIC, SIC, HIC and NIC into a cholecystokinin-B/gastrin receptor antagonist
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The preparation and biological properties of a conformationally constrained series of cholecystokinin-B/gastrin receptor ligands are described. The membered ring (Nic) derivative was found to be as active at these receptors as an unconstrained phenylalani
- Gibson, Susan E.,Guillo, Nathalie,Kalindjian, S. Barret,Tozer, Matthew J.
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p. 1289 - 1292
(2007/10/03)
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