Antagonists design

Endomorphin-2 (Tyr-Pro-Phe-NH ), a potent and selective MOR agonist, was used as a template for MOR antagonist design [54,55]. Replacing the N-terminal tyrosine residue with 2,6-dimethyltyrosine... 

Kiyama, R., Honma, T., Hayashi, K., Ogawa, M., Hara, M., Fujimoto, M., and Fujishita, T. Angiotensin II receptor antagonists. Design, synthesis, and in vitro evaluation of dibenzo[a,d]cycloheptene and dibenzo[b,f oxepin derivatives. 

Figure 6. A minimum energy structure of the transannular bridged analog of the GnRH cyclic antagonist designed to constrain the conformation to that found for the parent cyclic antagonist. The Q -carbons of Ser and Pro have been linked by an ethylene bridge to accomplish this.

NK3 antagonists design, svnthesis, binding to NK receptors solution, library [247 ... 

Figure 1.14 Schematic illustration of the B2 receptor antagonist design approach utilized by Fujisawa Pharmaceutical [64-66].

V. J. Hruby, G. Han, M. E. Hadley, Design and bioactivities of melanotropic peptide agonist and antagonists design based on a conformationally constrained somatostatin template. Lett. Pept. Sci. 1998, 5,117-120. 

FIGURE 16.21 Selectin antagonists designed to be preorganized in the bioactive conformation. 

Krogsgaard-Larsen. P. er al. (1994) GABAa receptor agonist, partial agonists and antagonists. Design and therapeutic prospects. / Med. C/ em., 37,2489-2505. 

NR ANTAGONISTS DESIGNED BASED ON THE HELIX 12-FOLDING INHIBITION HYPOTHESIS... 

Fibrinogen Receptor Antagonists Design and Clinical Applications... 

Minarini, A., Budriesi, R Chiarini. A., Leonard , A., Melchiorre, C 1998. Search for a,-adrenoceptor subtypes selective antagonists design, synthesis and biological activity of cystazosin, an anj-adren-oceptor antagonist. Bioorg. Med. Chem. Lett. 8, 1353-1358. 

Imidazole-5-Acrylic Acids Potent Nonpeptide Angiotensin II Receptor Antagonists Designed Using a Novel Peptide Pharmacophore Model. 

Mahesh R, Devadoss T, Pandey DK, Bhatt S (2011) Discovery of new anti-depressants from structurally novel 5-HT3 receptor antagonists design, synthesis and pharmacological evaluation of 3-ethoxyquinoxalin-2-carboxamides. Bioorg Med Chem Lett 21(4) 1253-1256. doi 10.1016/j.bmcl.2010.12.064... 

Gavande N, Yamamoto I, Salam NK, Ai TH, Burden PM, Johnston GAR, Hanrahan JR, Chebib M. Novel cyclic phosphinic acids as GABA p receptor antagonists design, synthesis, and pharmacology. ACS Med. Chem. Lett. 2011 2 11-16. 

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