Skip to main content

Abstract

The discovery of benzodiazepines (BZs) 1and their receptors have opened a new era in the discovery and characterization of drugs acting on the central nervous system (CNS). The pioneering and explorative synthetic work

of Sternbach in the early days of the BZ era led to the development of compound 2with its unusual pharmacological profile. The story of its development as narrated by Sternbach himself is very interesting [1a-c]. While its structure was studied by Sternbach and Reeder [1d], its sophisticated pharmacological tests were done by Randall and his staff [2]. It was given the generic name chlordiazepoxide and was launched under the trade name Librium®. The synthesis of this compound was rapidly followed by its derivative diazepam 3, which was given the trade name Valium®. These two drugs, which appeared on the market in rapid succession, soon became the most frequently prescribed CNS drugs. The success of these two drugs led Sternbach and his group to synthesize a number of related products (for examples see papers in ref. [3]) and, by the end of 1983, about 35 benzodiazepine drugs were available for therapy. The BZ drugs have a wide range of therapeutic applications [4].

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. L.H. Sternbach: Medicinal Chemistry Award Address presented at the 16th Medicinal Chemistry Symposium in Kalamazoo, Mich., June 20, 1978;

    Google Scholar 

  2. L.H. Sternbach: J. Med. Chem. 22, 1 (1978);

    Google Scholar 

  3. L.H. Sternbach: Agents Actions 2, 193 (1972);

    PubMed  CAS  Google Scholar 

  4. L. H. Sternbach and E. Reeder: J. Org. Chem. 26, 1111 (1961).

    CAS  Google Scholar 

  5. L.O. Randall: Dis. Nerv. Syst., Suppl. 7, 22, Sect. 2 (1961);

    Google Scholar 

  6. L.O. Randall, W. Schallek, G.A. Heise, E.E Keith, and R.E. Bagdon: J. Pharm. Exp. Ther. 129, 163 (1960).

    CAS  Google Scholar 

  7. L.H. Sternbach, E. Reeder, O. Keller, and W. Metlesics: J. Org. Chem. 26, 4488 (1961), and additional unpublished results;

    CAS  Google Scholar 

  8. L.H. Sternbach and E. Reeder: J. Org. Chem. 26, 4936 (1961);

    CAS  Google Scholar 

  9. L.H. Sternbach and L.O. Randall: CNS Drugs, Symp., Hyderabad, India, 53 (1966);

    Google Scholar 

  10. L.H. Sternbach, R.I. Fryer, W. Metlesics, E. Reeder, G. Sach, C. Saucy, and A. Stempel: J. Org. Chem. 27, 3788 (1962);

    CAS  Google Scholar 

  11. L.H. Sternbach, L.O. Randall, R. Banziger, and H. Lehr, in: Medicinal Research Series, Vol. 2, Ed. A. Burger, Marcel Dekker, New York, N.Y. (1968), p. 237;

    Google Scholar 

  12. N.W. Gilman and L.H. Sternbach: J. Heterocycl. Chem. 8, 297(1971);

    CAS  Google Scholar 

  13. R.I. Fryer, R.A. Schmidt, and L.H. Sternbach: J. Pharm. Sci. 53, 264 (1964);

    PubMed  CAS  Google Scholar 

  14. R. Kalish, E. Broger, G.F. Field, T. Anton, T.V. Steppe, and L.H. Sternbach: J. Heterocycl. Chem. 12, 49 (1975);

    CAS  Google Scholar 

  15. G.A. Archer, R.I. Kalish, R.Y. Ning, B.C. Sluboski, A. Stempel, T.V. Steppe, and L.H. Sternbach: J. Med. Chem. 20, 1312 (1977).

    PubMed  CAS  Google Scholar 

  16. L.E. Hollister, in: Pharmacology of Benzodiazepines. Ed. E. Usdin, Verlag Chemie, Weinheim (1983), p. 29.

    Google Scholar 

  17. H. Möhler and T. Okada: Science 198, 849 (1977);

    PubMed  Google Scholar 

  18. R.E Squires and C. Braestrup: Nature 266, 732 (1977).

    PubMed  CAS  Google Scholar 

  19. H. Möhler and J. Okada: Life Sci. 20, 2101 (1977);

    PubMed  Google Scholar 

  20. C. Braesttup, and R.F. Squires: Proc. Natl. Acad. Sci., USA 74, 3805 (1977).

    Google Scholar 

  21. W. Haefely, L. Pieri, P. Polc and R. Schaffner, in: Handbook of Experimental Pharmacology, Vol. 55/II, Eds. F. Hoffmeister and Stille, Springer Verlag, Berlin (1981), p. 13.

    Google Scholar 

  22. W. Haefely and P. Polc, in: Benzodiazepine-GABA Receptor and Chloride Channels: Structure and Functional Properties. Eds. R.W. Olson and J.C. Venter, Lis, New York (1986), p. 97.

    Google Scholar 

  23. A. Nistri and A. Constani: Neuropharmacology 17, 127 (1978).

    PubMed  CAS  Google Scholar 

  24. M.A. Simmonds: Trends. Neurosci. 6, 279 (1983).

    CAS  Google Scholar 

  25. M.A. Simmonds, in: Actions and Interactions of GABA and Benzodiazepines. Ed. N.G. Bowery, Raven Press, New York (1984), p. 27.

    Google Scholar 

  26. N.G. Bowery, D.R. Hill, and A.L. Hudson: Br. J. Pharmacol. 78, 191 (1983).

    PubMed  CAS  Google Scholar 

  27. N.G. Bowery, D.R. Hill, A.L. Hudson, G.W. Price, M.J. Turnbull, and G. P. Wilkin, in: Actions and Interactions of GABA and Benzodiazepines. Ed. N.G. Bowery, Raven Press, New York (1984), p. 81.

    Google Scholar 

  28. R. Sherman-Gold and Y. Dudai: FEBS letters 131, 313 (1981).

    PubMed  CAS  Google Scholar 

  29. T.P. Bürch and M.K. Ticku: Proc. Natl. Acad. Sci., USA 78, 3945 (1981).

    PubMed  Google Scholar 

  30. R. Sherman-Gold and Y. Dudai: Neurochem. Res. 8, 853 (1983).

    PubMed  CAS  Google Scholar 

  31. W. Haefely, E. Kyburz, M. Gerecke, and H. Möhler, in: Advances in Drug Research, Vol. 14, Ed. B. Testa, Academic Press, London (1985), p. 165.

    Google Scholar 

  32. D. Römer, H.H. Büscher, R.C. Hill, R. Maurer, I.J. Zeugner, W. Benzon, E. Finner, W. Milkowski, and P.W. Thies: Life Sci. 31, 1217 (1982).

    PubMed  Google Scholar 

  33. D. Römer, H.H. Büscher, R.C. Hill, R. Maurer, T.F. Petscher, H. Zeugner, W. Benson, E. Finner, W. Milkowski, and P.W. Thies: Nature 298, 759 (1982).

    PubMed  Google Scholar 

  34. H. Kley, U. Scheidemantel, B. Bering, and W. Müller: Eur. J. Pharmacol. 87, 503 (1983).

    PubMed  CAS  Google Scholar 

  35. W.H. Haefely: Chimia 41, 389 (1987).

    CAS  Google Scholar 

  36. R.I. Fryer, in: Comprehensive Medicinal Chemistry, Vol. 3, Eds. C. Hansch, P.G. Sammes, and J.B. Taylor, Pergamon Press, New York (1990), p. 539.

    Google Scholar 

  37. P. Pole, E. Bonetti, R. Schaffner, and W. Haefely: Arch. Pharmacol. 321, 260 (1982).

    Google Scholar 

  38. R.I. Fryer, N.W. Gilman, V. Madison, and A. Walser, in: Proceedings of the VIIIth International Symposium on Medicinal Chemistry, Vol. 2, Eds. R. Dahlbom and J.L. Nilsson, Swedish Pharmaceutical Press, Stockholm (1985), p. 265.

    Google Scholar 

  39. C. Braestrup, M. Nielsen, and T. Honore, in: CNS Receptors: From Molecular Pharmacology to Behaviour. Eds. P. Mandel and F.V. DeFeudis, Raven Press, New York (1983), p. 237.

    Google Scholar 

  40. E. Kyburz: Pharm. Weekl. 121, 893 (1986).

    CAS  Google Scholar 

  41. M. Cain, R. Weber, F. Guzman, J. Cook, J. Barker, K. Rice, J. Crawley, S. Paul, and P. Skolnick: J. Med. Chem. 25, 1081 (1982).

    PubMed  CAS  Google Scholar 

  42. S. Cooper: Trends Pharmacol. Sci. 7, 210 (1986).

    Google Scholar 

  43. C. Braestrup, T. Honore, M. Nielsen, E. Petersen and L. Jensen: Biochem. Pharmacol. 33, 859 (1984).

    PubMed  CAS  Google Scholar 

  44. P. Wood, P. Loo, A. Braunwalder, and N. Yokoyama: J. Pharmacol. Exp. Then 231, 572 (1984).

    CAS  Google Scholar 

  45. N. Yokohama, B. Ritter, and A.D. Neubert: J. Med. Chem. 12, 337 (1982).

    Google Scholar 

  46. C. Boast, E. Snowhill, and J. Smike: J. Pharmacol. Biochem. Behav. 23, 639 (1985).

    CAS  Google Scholar 

  47. A.J. Czernik, B. Tetrack, H. Kalinsky, S. Psychoyos, W. Cash, C. Tsai, R. Rinehart, F. Granat, R. Lovell, D. Brundish, and R. Wade: Life Sci. 30, 363 (1982).

    PubMed  CAS  Google Scholar 

  48. J. Albright, D. Moran, W. Wright, Jr., J. Collins, B. Beer, A. Lippa, and E. Greenblatt: J. Med. Chem. 4, 592 (1981).

    Google Scholar 

  49. K. Biziere, J. Bourguignon, J. Chambon, M. Heaulme, A. Perio, S. Tebib, and CG. Wermuth: Br. J. Pharmacol. 90, 1983 (1987).

    Google Scholar 

  50. S. Tebib, J.-J. Bourguignon, and C.-G. Wermuth: J. Computer-Aided Mol. Design 1, 153 (1987).

    CAS  Google Scholar 

  51. R.I. Fryer, in: The Benzodiazepines: From Molecular Biology to Clinical Practice. Ed. E. Costa, Raven Press, New York (1983), p. 7.

    Google Scholar 

  52. R.I. Fryer, C. Cook, N.W. Gilman, and A. Walsher: Life Sci. 39, 1947 (1986).

    PubMed  CAS  Google Scholar 

  53. J.C. Fong, K. Okada, and M. Goldstein: Eur. J. Pharmacol. 77, 57 (1982).

    PubMed  CAS  Google Scholar 

  54. M. Trudell, A. Basile, H. Shannon, P. Skolnick, and J.M. Cook: J. Med. Chem. 30, 456 (1987).

    PubMed  CAS  Google Scholar 

  55. H. Takeda, H. Shindo, T. Sasatani, N. Chomei, A. Matsushita, M. Eigyo, K. Kawasaki, S. Murata, Y. Takahara, and H. Shintaku: J. Med. Chem. 31, 1738 (1988).

    Google Scholar 

  56. M. Allen, T. Hagen, M. Trudell, P. Codding, P. Skolnick, and J.M. Cook: J. Med. Chem. 31, 1854 (1988).

    PubMed  CAS  Google Scholar 

  57. L.H. Sternbach, L.O. Randall, and S.R. Gustavson: Psychopharmacological Agents 1, 137 (1964).

    Google Scholar 

  58. L.H. Sternbach, L.O. Randall, R. Banziger, and H. Lehr, in: Drugs Affecting the Nervous System. Ed. A. Burger, Dekker, New York (1968), p. 237.

    Google Scholar 

  59. L.H. Sternbach, in: The Benzodiazepines. Eds. S. Garatlini, E. Mussini, and L.O. Randall, Raven Press, New York (1973), p. 1.

    Google Scholar 

  60. L.H. Sternbach: Prog. Drug Res. 22, 229 (1978).

    PubMed  CAS  Google Scholar 

  61. R.I. Fryer, W. Leimgruber, and Trybulski: J. Med. Chem. 25, 1050 (1982).

    PubMed  CAS  Google Scholar 

  62. P.A. Borea, G. Gilli, and V. Bertolasi: II Farmaco, Ed. Sci. 34, 1073 (1979).

    CAS  Google Scholar 

  63. P.G. Baraldi, S. Manfredini, V. Periotto, D. Simino, M. Guarneri, and P.A. Borea: J. Med. Chem. 28, 683 (1985).

    PubMed  CAS  Google Scholar 

  64. S.P. Gupta, R.N. Saha, and V. Mulchandani: J. Molec. Recog. 5, 75 (1992).

    CAS  Google Scholar 

  65. F. Watjen, R. Baker, M. Engelstoff, R. Herbert, A. MacLeod, A. Knight, K. Merchant, J. Moseley, J. Saunders, C.J. Swain, E. Wong, and J.P. Springer: J. Med. Chem. 32, 2282 (1989).

    PubMed  CAS  Google Scholar 

  66. Z-Q. Gu, B.R. de Costa, G. Wong, K.C. Rice, and P. Skolnick: J. Label. Compd. Radiopharm. 31, 1049 (1992).

    CAS  Google Scholar 

  67. S. Ananthan, S.D. Clayton, S.E. Ealick, G. Wong, G.E. Evoniuk, and P. Skolnick: J. Med. Chem. 36, 479 (1993).

    PubMed  CAS  Google Scholar 

  68. Z.-Q. Gu, G. Wong, C. Dominguez, B.R. de Costa, K.C. Rice, and P. Skolnick: J. Med. Chem. 36, 1001 (1993).

    PubMed  CAS  Google Scholar 

  69. G. Wong, K.E. Koehler, P. Skolnick, Z.-Q. Gu, S. Ananthan, P. Schönholzer, W. Hunkler, W. Zhang, and J.M. Cook: J. Med. Chem. 36, 1820 (1993).

    PubMed  CAS  Google Scholar 

  70. R.I. Fryer, P. Zhang, K.-Y. Lin, R.B. Upasani, G. Wong, and P. Skolnick: Med. Chem. Res. 3, 183 (1993).

    CAS  Google Scholar 

  71. D.M. Turner, D.W. Sapp, and R.W. Olsen: J. Pharmacol. Exp. Ther. 247, 1236 (1991).

    Google Scholar 

  72. G. Wong and P. Skolnick: Eur. J. Pharm. Mol. Pharm. Sec. 225, 63 (1992).

    CAS  Google Scholar 

  73. G. Wong, P. Skolnick, J. Katz, and J. Witkin: J. Pharm. Ex. Ther., in press. (1994).

    Google Scholar 

  74. E.R. Korpi, M. Uusi-Oukari, and K. Wegeluis: Eur. J. Pharm. 213, 323 (1992).

    CAS  Google Scholar 

  75. R.C. Sharma, P. Singh, and T.N. Ojha: Res. Commun. Chem. Pathol. Pharmacol. 80, 357(1993).

    PubMed  CAS  Google Scholar 

  76. V. Nacci and I. Fiorini: II Farmaco, Ed. Sci. 38, 112 (1983).

    CAS  Google Scholar 

  77. V. Nacci, I. Fiorini, S. Vomero, I. Taddei, and E. Taddei: II Farmaco, Ed. Sci. 39, 289 (1984).

    CAS  Google Scholar 

  78. V. Nacci, I. Fiorini, A. Garofalo, and A. Cagnotto: II Farmaco, Ed. Sci. 45, 545 (1990).

    CAS  Google Scholar 

  79. I. Fiorini, V. Nacci, S.M. Ciani, A. Garofalo, G. Campiani, L. Savini, E. Novellino, G. Greco, P. Bernasconi, and T. Mennini: J. Med. Chem. 37, 1427 (1994).

    PubMed  CAS  Google Scholar 

  80. H. Rommelspacher, C. Nanz, H.O. Borbe, K.J. Feshske, W.E. Müller, and U. Wollert: Naunyn-Schmiedeberg’s Arch. Pharmacol. 314, 97 (1980).

    CAS  Google Scholar 

  81. H. Rommelspacher, C. Nanz. H.O. Borbe, K.J. Feshske, W.E. Müller, and U. Wollert: Eur. J. Pharmacol. 70, 409 (1981).

    PubMed  CAS  Google Scholar 

  82. W.E. Müller, K.J. Fehske, H.O. Borbe, U. Wollert, C. Nanz, and H. Rommelspacher: Pharmacol. Biochem. Behav. 14, 693 (1981).

    PubMed  Google Scholar 

  83. H. A. Robertson, G.B. Baker, R.T Coutts, A. Benderly, RA. Locock, and I.L. Martin: Eur. J. Pharmacol. 76, 281 (1981).

    PubMed  CAS  Google Scholar 

  84. C. Braestrup, M. Nielsen, and C.E. Olsen: Proc. Natl Acad. Sci., USA 77, 2288 (1980).

    PubMed  CAS  Google Scholar 

  85. C. Braestrup and M. Nielsen: J. Neurochem. 37, 333 (1981).

    PubMed  CAS  Google Scholar 

  86. K.J. Fenske, I. Zube, H.O. Borbe, U. Wollert, and W.E. Müller: Naunyn-Sehmiedeberg’s Arch. Pharmacol. 319, 172 (1982).

    Google Scholar 

  87. F.J. Ehlert, W.R. Roeske, and H.I. Yamamura: Life Sci. 29, 235 (1981).

    PubMed  CAS  Google Scholar 

  88. J.D. Hirsch, R.L. Kochman, and P R. Sumner: Mol. Pharmacol. 21, 618 (1982).

    PubMed  CAS  Google Scholar 

  89. M. Cain, R.W. Weber, F. Guzman, J.M. Cook, S.A. Barker, K.C. Rice, J.N. Crawley, S.M. Paul, and P. Skolnick: J. Med. Chem. 25, 1081 (1982).

    PubMed  CAS  Google Scholar 

  90. K.P. Lippke, W.G. Schunack, W. Wenning, and W.E. Müller: J. Med. Chem. 26, 499 (1983).

    PubMed  CAS  Google Scholar 

  91. F. Guzman, M. Cain, P. Larscheid, T. Hagen, J.M. Cook, M. Schweri, P. Skolnick, and S.M. Paul: J. Med. Chem. 27, 564 (1984).

    PubMed  CAS  Google Scholar 

  92. G. Dorey, G. Poissonnet, M.-C. Potier, L.P. de Carvalho, P. Venault, G. Chapouthier, J. Rossier, P. Potier, and R.H. Dodd: J. Med. Chem. 32, 1799 (1989).

    PubMed  CAS  Google Scholar 

  93. R.C. Sharma, T.N. Ojha, S. Tiwari, and P. Singh: Drug Des. Discov. 9, 135 (1992).

    PubMed  CAS  Google Scholar 

  94. T.H. Hagen, P. Skolnick, and J.M. Cook: J. Med. Chem. 30, 750 (1987).

    PubMed  CAS  Google Scholar 

  95. S.P. Hollinshead, M.L. Trudell, P. Skolnick, and J.M. Cook: J. Med. Chem. 33, 1062 (1990).

    PubMed  CAS  Google Scholar 

  96. H.O. Villar and G.H. Loew: Int. J.Quantum Chem., Quantum Biol. Symp. 16, 261 (1989).

    CAS  Google Scholar 

  97. G.H. Loew, J.R. Nienow, J.A. Lawson, L. Toll, and E.T. Uyeno: Mol. Pharmacol. 28, 17 (1985).

    PubMed  CAS  Google Scholar 

  98. G.H. Loew, J.R. Nienow, and M. Poulsen: Mol. Pharmacol. 26, 19 (1984).

    PubMed  CAS  Google Scholar 

  99. R.H. Dodd, C. Ouannès, M.-C. Potier, L.P. de Carvalho, J. Rossier, and P. Potier: J. Med. Chem. 30, 1248 (1987).

    PubMed  CAS  Google Scholar 

  100. M.L. Trudell, S.L. Lifer, Y.-C. Tan, M.J. Martin, L. Deng, P. Skolnick, and J.M. Cook: J. Med. Chem. 33, 2412 (1990).

    PubMed  CAS  Google Scholar 

  101. N. Yokoyama, B. Ritter, and A.D. Neubert: J. Med. Chem. 25, 337 (1982).

    PubMed  CAS  Google Scholar 

  102. L. Cecchi, F. Melani, G. Palazzino, G. Filacchioni, C. Martini, E. Pennacchi, and A. Lucacchini: II Farmaco, Ed. Sci. 40, 509 (1985).

    CAS  Google Scholar 

  103. F. Melani, L. Cecchi, G. Palazzino, G. Filacchioni, C. Martini, E. Pennacchi, and A. Lucacchini: J. Med. Chem. 29, 291 (1986).

    PubMed  CAS  Google Scholar 

  104. F. Melani, L. Cecchi, G. Palazzino, G. Filacchioni, C. Martini, E. Penacchi, and A. Lucacchini: J. Pharm. Sci. 75, 1175 (1986).

    PubMed  CAS  Google Scholar 

  105. G. Palazzino, L. Cecchi, F. Melani, V. Colotta, G. Filacchioni, C. Martini, and A. Lucacchini: J. Med. Chem. 30, 1737 (1987).

    PubMed  CAS  Google Scholar 

  106. V. Colotta, L. Cecchi, F. Melani, D. Catarzi, G. Filacchioni, C. Martini, G. Gianaccini, M. Tonelli, and A. Lucacchini: Drug Des. Deliv. 8, 325 (1992).

    CAS  Google Scholar 

  107. H.O. Villar, E.T. Uyeno, L. Toll, W. Polgar, M.F. Davies, and G.H. Loew: Mol. Pharmacol. 36, 589 (1989).

    PubMed  CAS  Google Scholar 

  108. G. Wong, Z.-Q. Gu, R.I. Fryer, and P. Skolnick: Med. Chem. Res. 2, 217 (1992).

    CAS  Google Scholar 

  109. R.I. Fryer, R. Rios, P. Zhang, Z.-Q. Gu, G. Wong, A.S. Basile, and P. Skolnick: Med. Chem. Res. 3, 122 (1993).

    CAS  Google Scholar 

  110. R.I. Fryer, P. Zhang, R. Rios, Z.-Q. Gu, A.S. Basile, and P. Skolnick: J. Med. Chem. 36, 1669 (1993).

    PubMed  CAS  Google Scholar 

  111. S. Takada, H. Shinde, T. Sasatani, N. Chomei, A. Matsushita, M. Eigyo, K. Kawasaki, S. Murata, Y. Takahara, and H. Shintaku: J. Med. Chem. 31, 1738 (1988).

    PubMed  CAS  Google Scholar 

  112. S. Shindo, S. Takada, S. Murata, M. Eigyo, and A. Matsushita: J. Med. Chem. 32, 1213 (1989).

    PubMed  CAS  Google Scholar 

  113. V. Colotta, L. Cecchi, F. Melani, G. Palazzino, and G. Filacchioni: Tetrahedron Letters 28, 5165 (1987).

    CAS  Google Scholar 

  114. V. Colotta, L. Cecchi, G. Filacchioni, F. Melani, G. Palazzino, C. Martini, G. Giannaccini, and A. Lucacchini: J. Med. Chem. 31, 1 (1988).

    PubMed  CAS  Google Scholar 

  115. V. Colotta, L. Cecchi, F. Melani, G. Palazzino, G. Filacchioni, C. Martini, G. Giannaccini, and A. Lucacchini: J. Pharm. Sci. 78, 239 (1989).

    PubMed  CAS  Google Scholar 

  116. V. Colotta, L. Cecchi, F. Melani, G. Filacchioni, C. Martini, S. Gelli, and A. Lucacchini: J. Pharm. Sci. 80, 276 (1991).

    PubMed  CAS  Google Scholar 

  117. S.P. Gupta, R.N. Saha, J.K. Gupta, and P. Singh: Res. Commun. Chem. Pathol. Pharmacol. 65, 119 (1989).

    PubMed  CAS  Google Scholar 

  118. P. Singh, T.N. Ojha, and R.C. Sharma: Res. Commun. Chem. Pathol. Pharmacol. 67, 151 (1990).

    PubMed  CAS  Google Scholar 

  119. P. Singh, T.N. Ojha, R.C. Sharma, and S. Tiwari: Indian J. Chem. 32B, 555 (1993).

    CAS  Google Scholar 

  120. S.P Gupta and Anitha Paleti: Communicated.

    Google Scholar 

  121. V. Colotta, L. Cecchi, F. Melani, G. Filacchioni, C. Martini, G. Giannaccini, and A. Lucacchini: J. Med. Chem. 33, 2646 (1990).

    PubMed  CAS  Google Scholar 

  122. L. Cecchi, V. Colotta, G. Filaccchioni, F. Melani, G. Palazzino, and A. Galli: II Farmaco, Ed., Sci. 42, 671 (1987).

    CAS  Google Scholar 

  123. L. Cecchi, V. Colotta, F. Melani, G. Palazzino, G. Filacchioni, C. Martini, G. Giannaccini, and A. Lucacchini: J. Pharm. Sci. 78, 437 (1989).

    PubMed  CAS  Google Scholar 

  124. M.S. Allen, P. Skolnick, and J.M. Cook: J. Med. Chem. 35, 368 (1992).

    PubMed  Google Scholar 

  125. V. Colotta, L. Cecchi, F. Melani, G. Filacchioni, C. Martini, S. Gelli, and A. Lucacchini: II Farmaco, Ed. Sci. 46, 1139 (1991).

    CAS  Google Scholar 

  126. J.E. Francis, W.D. Cash, B.S. Barbaz, P.S. Bernard, R.A. Lovell, G.C. Mazzenga, R.C. Friedman, J.L. Hyun, A.F. Braunwalder, P.S. Loo, and D.A. Bennett: J. Med. Chem. 34, 281 (1991).

    PubMed  CAS  Google Scholar 

  127. V. Colotta, L. Cecchi, D. Catarzi, G. Conti, G. Filacchioni, C. Martini, L. Giusti, and A. Lucacchini: II Farmaco, Ed. Sci. 48, 1051 (1993).

    CAS  Google Scholar 

  128. D. Catarzi, L. Cecchi, V. Colotta, F. Melani, G. Filacchioni, C. Martini, L. Giusti, and A. Lucacchini: II Farmaco, Ed. Sci. 48, 1065 (1993).

    CAS  Google Scholar 

  129. D. Catarzi, L. Cecchi, V. Colotta, F. Melani, G. Filacchioni, C. Martini, L. Giusti, and A. Lucacchini: J. Med. Chem. 37, 2846 (1994).

    PubMed  CAS  Google Scholar 

  130. G. Targia, E. Occelli, E. Toja, D. Barone, N. Corsico, L. Gallico, and F. Luzzani: J. Med. Chem. 31, 1115(1988).

    Google Scholar 

  131. D. Catarzi, L. Cecchi, V. Colotta, G. Conti, F. Melani, G. Filacchioni, C. Martini, L. Giusti, and A. Lucacchini: II Farmaco, Ed.Sci. 48, 447 (1993).

    CAS  Google Scholar 

  132. F. Melani, L. Cecchi, V. Colotta, G. Filacchioni, C. Martini, G. Giannaccini, and A. Lucacchini: II Farmaco, Ed. Sci. 44, 585 (1989).

    CAS  Google Scholar 

  133. J.E. Francis, D.A. Bennett, J.L. Hyun, S.L. Rovinski, C.L. Amrick, P.S. Loo, D. Murphy, R.F. Neale, and D.E. Wilson: J. Med. Chem. 34, 2899 (1991).

    PubMed  CAS  Google Scholar 

  134. J.L. Kelley, E.W. McLean, R.M. Ferris, and J.L. Howard: J. Med. Chem. 32, 1020 (1989).

    PubMed  CAS  Google Scholar 

  135. J.L. Kelley, E.W. McLean, J.A. Linn, M.P Krochmal, R.M. Ferris, and J.L. Howard: J. Med. Chem. 33, 196 (1990).

    PubMed  CAS  Google Scholar 

  136. J.L. Kelley, E.W McLean, R.M. Ferris, and J.L. Howard: J. Med. Chem. 33, 1910 (1990).

    PubMed  CAS  Google Scholar 

  137. J.L. Kelley, E.W McLean, R.M. Ferris, and J.L. Howard: J. Heterocyclic Chem. 28, 1099 (1991).

    CAS  Google Scholar 

  138. R.N. Saha, J. Meera, N. Agrawal, and S.P Gupta: Drug Des. Deliv. 7, 219 (1991).

    PubMed  CAS  Google Scholar 

  139. S.P. Gupta and V. Mulchandani: Indian J. Biochem. Biophys. 30, 181 (1993).

    PubMed  CAS  Google Scholar 

  140. C. Martini, T. Gervasio, A. Lucacchini, A.D. Settimo, G. Primofiore, and A.M. Martini: J. Med. Chem. 28, 506 (1985).

    PubMed  CAS  Google Scholar 

  141. G. Primofiore, A.M. Marini, F.D. Settimo, C. Martini, A. Bardellini, G. Giannaccini, and A. Lucacchini: J. Med. Chem. 32, 2514 (1989).

    PubMed  CAS  Google Scholar 

  142. A.M. Bianucci, A.D. Settimo, F.D. Settimo, G. Primofiore, C. Martini, G. Giannaccini, and A. Lucacchini: J. Med. Chem. 35, 2214 (1992).

    PubMed  CAS  Google Scholar 

  143. G.M. Crippen: Mol. Pharmacol. 22, 11 (1982).

    PubMed  CAS  Google Scholar 

  144. P.W. Codding and A.K. Muir: Mol. Pharmacol. 28, 178 (1985).

    PubMed  CAS  Google Scholar 

  145. M.S. Allen, Y.-C. Tan, M.L. Trudell, K. Narayanan, L.R. Schindler, M.J. Martin, C. Schultz, T.J. Hagen, K.F. Koehler, P.W. Codding, P. Skolnick, and J.M. Cook: J. Med. Chem. 33, 2343 (1990).

    PubMed  CAS  Google Scholar 

  146. P.A. Borea, G. Gilli, V. Bertolasi, and V. Ferretti: Mol. Pharmacol. 31, 334 (1987).

    PubMed  CAS  Google Scholar 

  147. M.S. Allen, A.J. LaLoggia, L.J. Dora, M.J. Martin, G. Costantino, T.J. Hagen, K.F. Koehler, P. Skolnick, and J.M. Cook: J. Med. Chem. 35, 4001 (1992).

    PubMed  CAS  Google Scholar 

  148. M.J. Martin, M.L. Trudell, H.D. Araúzo, M.S. Allen, A.J. LaLoggia, L. Deng, C.A. Schultz, Y.-C. Tan, Y Bi, K. Narayanan, L.J. Dorn, K.F. Koehler, P. Skolnick, and J.M. Cook: J. Med. Chem. 35, 4105 (1992).

    PubMed  CAS  Google Scholar 

  149. W. Zhang, K.F. Koehler, B. Harris, P. Skolnick, and J.M. Cook: J. Med. Chem. 37, 745 (1994).

    PubMed  CAS  Google Scholar 

  150. H. Diaz-Araúzo, G.E. Evoniuk, P. Skolnick, and J.M. Cook: J. Med. Chem. 34, 1754 (1991).

    PubMed  Google Scholar 

  151. A. Yliniemelä, J. Gynther, K. Konschin, H. Tylli, and J. Rouvinen: Int. J. Quantum. Chem., Quantum Biol. Symp. 16, 273 (1989).

    Google Scholar 

  152. G. Georges, D.P. Vercauteren, D.J. Vanderveken, R. Horion, G. Evrard, J.G. Fripiat, J.-M. Andre, and F. Durant: Int. J. Quantum Chem., Quantum Biol. Symp. 17, 1 (1990).

    CAS  Google Scholar 

  153. H.O. Villar and G. H. Loew: Int. J. Quantum Chem., Quantum Biol. Symp. 18, 131 (1991).

    CAS  Google Scholar 

  154. H.O. Villar, M.F. Davies, G.H. Loew, and P.A. Maguire: Life Sci, 48, 593 (1991).

    PubMed  CAS  Google Scholar 

  155. S.P Gupta: Indian J. Chem. 33B, 105 (1994).

    CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1995 Birkhäuser Verlag, Basel (Switzerland)

About this chapter

Cite this chapter

Gupta, S.P. (1995). Recent advances in benzodiazepine receptor (BZR) binding studies. In: Jucker, E. (eds) Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des Recherches Pharmaceutiques. Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des recherches pharmaceutiques, vol 45. Birkhäuser Basel. https://doi.org/10.1007/978-3-0348-7164-8_3

Download citation

  • DOI: https://doi.org/10.1007/978-3-0348-7164-8_3

  • Publisher Name: Birkhäuser Basel

  • Print ISBN: 978-3-0348-7166-2

  • Online ISBN: 978-3-0348-7164-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics