PD 176252 - The first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 18, 1998, Pages 2589-2594

  Ashwood, V ^a   Brownhill, V ^a   Higginbottom, M ^a   Horwell, D C ^a   Hughes, J ^a   Lewthwaite, R A ^a   McKnight, A T ^a   Pinnock, R D ^a   Pritchard, M C ^a   Suman Chauhan, N ^a   Webb, C ^a   Williams, S C ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BOMBESIN ANTAGONIST; GASTRIN ANTAGONIST; GASTRIN RELEASING PEPTIDE; NEUROMEDIN B; PD 176252; UNCLASSIFIED DRUG;

ANXIETY; ARTICLE; DEPRESSION; DRUG DESIGN; DRUG SELECTIVITY; DRUG SYNTHESIS; GASTRIN RELEASE; RECEPTOR AFFINITY; SATIETY; STEREOTYPY; STRUCTURE ACTIVITY RELATION; THERMOREGULATION;

ANIMALS; GASTRIN-RELEASING PEPTIDE; HUMANS; INDOLES; KINETICS; LIGANDS; MODELS, CHEMICAL; NEUROKININ B; RATS; RECEPTORS, BOMBESIN; SPECIES SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032558515     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00462-4     Document Type: Article

References (22)

1. 1. Eden, J. M. ; Hall, M. D. ; Higginbottom, M.; Horwell, D. C. ; Howson, W.; Hughes, J.; Jordan, R. E.; Lewthwaite, R. A.; Martin, K.; McKnight, A. T.; O'Toole, J. C.; Pinnock, R. D. ; Pritchard, M. C. ; Suman-Chauhan, N.; Williams, S. C. Bioorg. Med. Chem. Lett. 1996, 6, 2617.
2. 2. a) For a recent review of this work see Horwell, D. C. Trends Biotechnol. 1995, 13, 132.
3. b) For a more detailed description of the peptoid design strategy see Boyle, S.; Guard, S.; Hodgson, J.; Horwell, D. C.; Howson, W.; Hughes, J.; McKnight, A.; Martin, K.; Pritchard, M. C.; Watling, K. J.; Woodruff, G. N. Bioorg. Med. Chem. 1994, 2, 101.
4. 3. For examples of CCK antagonists see Horwell, D.C.; Hughes, J.; Hunter, J.C.; Pritchard, M.C.; Richardson, R.S.; Roberts, E.; Woodruff, G.N. J. Med. Chem. 1991, 34, 404. For CCK agonists see Burgaud, B.G.M.; Horwell, D.C.; Pritchard, M.C.; Bernad, N.; Martinez, J. Tetrahedron: Asymmetry 1995, 6, 1081.
5. 3. For examples of CCK antagonists see Horwell, D.C.; Hughes, J.; Hunter, J.C.; Pritchard, M.C.; Richardson, R.S.; Roberts, E.; Woodruff, G.N. J. Med. Chem. 1991, 34, 404. For CCK agonists see Burgaud, B.G.M.; Horwell, D.C.; Pritchard, M.C.; Bernad, N.; Martinez, J. Tetrahedron: Asymmetry 1995, 6, 1081.
6. 4. See Boden, P.; Eden, J. M.; Hodgson, J.; Horwell, D. C.; Pritchard, M. C.; Raphy, J.; Suman-Chauhan, N. Bioorg. Med. Chem. Lett. 1995, 5, 1773 and references cited therein.
7. 5. See Chapter 2 in Dutta, A. S. Small Peptides : Chemistry, Biology and Clinical Studies, (1993) Pharmacochemistry Library Vol. 19 (Timmerman, H., ed), Elsevier.
8. 6. Battey, J.; Wada, E. Trends Neurosci. 1991, 14, 524.
9. 7. a) Lebacq-Verheyden, A.; Trepel, J.; Sausville, E.; Battey, J. Handbook of Experimental Pharmacology 1990, 95 (Part II), 71;
10. b) Kent, P.; Anisman, H.; Merali, Z. Life Sci. 1997, 62, 103;
11. c) Plamondon, H.; Moody, T. W.; Merali, Z. Soc. Neurosci. 1996, 22, 181.13.
12. 8. Gorbulev, V.; Akhundova, A.; Buchner, H.; Fahrenholz, F. Eur. J. Biochem. 1992, 208, 405.
13. 9. Nagalla, S. R.; Barry, B. J.; Creswick, K. C.; Eden, P.; Taylor, J. T.; Spindel, E. R. Proc. Natl. Acad. Sci. USA 1995, 92, 6205.
14. 10. a) Jensen, R. T.; Coy, D. H.; Trends Pharmacol. Sci. 1991, 12, 13;
15. b) Mantey, S. A.; Weber, H. C.; Sainz, E.; Akeson, M.; Ryan, R. R.; Pradhan, T. K.; Searles, R. P.; Spindel, E. R.; Battey, J. F.; Coy, D. H.; Jensen, R. T. J. Biol. Chem. 1997, 272, 26062.
16. 11. The structures of relatively low affinity non-peptide bombesin ligands have been disclosed: Valentine, J. J.; Nakanishi, S.; Hageman, D. L.; Snider, R. M.; Spencer, R. W.; Vinick, F. J. Bioorg. Med. Chem. Lett. 1992, 2, 333 and Mihara, S.; Hara, M.; Nakamura, M.; Sakurawi, K.; Tokura, K.; Fujimoto, M.; Fukai, T.; Nomura, T. Biochem. Biophys. Res. Comm. 1995, 213, 594.
17. 11. The structures of relatively low affinity non-peptide bombesin ligands have been disclosed: Valentine, J. J.; Nakanishi, S.; Hageman, D. L.; Snider, R. M.; Spencer, R. W.; Vinick, F. J. Bioorg. Med. Chem. Lett. 1992, 2, 333 and Mihara, S.; Hara, M.; Nakamura, M.; Sakurawi, K.; Tokura, K.; Fujimoto, M.; Fukai, T.; Nomura, T. Biochem. Biophys. Res. Comm. 1995, 213, 594.
18. 12. Topliss, J. G. J. Med. Chem. 1972, 15, 1006.
19. 13. Suman-Chauhan, N.; Hall, M.; Franks, R.; Webdale, L.; Chilvers, H.; Pinnock, R. D.; Woodruff, G. N. Br. J. Pharmacol. 1995, 116, 22P.
20. 14. Guard, S.; Watling, K. J.; Howson, W. Eur. J. Pharmacol. 1993, 240, 177.
21. 15. Jordan, R. E.; Smart, D.; Grimson, P.; Suman-Chauhan, N.; McKnight, A. T. Br. J. Pharmacol. 1998, (in press).
22. 16. Pinnock, R. D.; Suman-Chauhan, N.; Chung, F. Z.; Webdale, L.; Madden, Z.; Hill, D. R.; Woodruff, G. N. Eur. J. Pharmacol. 1994, 269,