Opiate aromatic pharmacophore structure-activity relationships in CTAP analogues determined by topographical bias, two-dimensional NMR, and biological activity assays
Topographically constrained analogues of the highly μ-opioid-receptor- selective antagonist CTAP (H-D-Phe-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2, 1) were prepared by solid-phase peptide synthesis. Replacement of the D-Phe residue with conformatio
Bonner, G. Gregg,Davis, Peg,Stropova, Dagmar,Edsall, Sidney,Yamamura, Henry I.,Porreca, Frank,Hruby, Victor J.
p. 569 - 580
(2007/10/03)
Design and Synthesis of Conformationally Constrained Somatostatin Analogues with High Potency and Specificity for μ Opioid Receptors
A series of cyclic, conformationally constrained peptides related to somatostatin were designed and synthesized in an effort to develop highly selective and potent peptides for the μ opioid receptor.The following new peptides were prepared and tested for
Pelton, John T.,Kazmierski, Wieslaw,Gulya, Karoly,Yamamura, Henry I.,Hruby, Victor J.
p. 2370 - 2375
(2007/10/02)
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