192133-95-2Relevant academic research and scientific papers
CCK2 receptor antagonists containing the conformationally constrained phenylalanine derivatives, including the new amino acid Xic
Gibson, Susan E,Guillo, Nathalie,Jones, Jerome O,Buck, Ildiko M,Kalindjian, S.Barret,Roberts, Sonia,Tozer, Matthew J
, p. 379 - 389 (2007/10/03)
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.
Incorporation of conformationally constrained phenylalanine derivatives TIC, SIC, HIC and NIC into a cholecystokinin-B/gastrin receptor antagonist
Gibson, Susan E.,Guillo, Nathalie,Kalindjian, S. Barret,Tozer, Matthew J.
, p. 1289 - 1292 (2007/10/03)
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
