Chemical design of peripherally acting compounds

W. Roy Jackson, Fred C. Copp, John D. Cullen, Frances J. Guyett, Ian D. Rae, Andrea J. Robinson, Helen Pothoulackis, Algirdas K. Serelis, Margaret Wong

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13 Citations (Scopus)

Abstract

1. Some guanidines, related in structure to mianserin and to 2‐methyl‐1,2,9,13b‐tetrahydro‐3H‐dibenz[c,f]irnadazo[l,5a]azepin‐3‐imine hydrobromide (WAL 801), have been synthesized and shown to be peripherally acting 5‐HT2 antagonists. Structurally related compounds but not bearing a charged ionic group have been shown to have central activity. 2. Computer‐aided molecular modelling has been used to establish a 5‐HT2 pharmacophore. 3. The principle of exclusion from the CNS by incorporating a highly polar group to a biologically active molecule has been extended to the design and synthesis of a peripherally acting analgesic.

Original languageEnglish
Pages (from-to)17-23
Number of pages7
JournalClinical and Experimental Pharmacology and Physiology
Volume19
Issue number1
DOIs
Publication statusPublished - 1 Jan 1992

Keywords

  • analgesics
  • peripherally acting drugs
  • S‐HT antagonists

Cite this

Jackson, W. R., Copp, F. C., Cullen, J. D., Guyett, F. J., Rae, I. D., Robinson, A. J., Pothoulackis, H., Serelis, A. K., & Wong, M. (1992). Chemical design of peripherally acting compounds. Clinical and Experimental Pharmacology and Physiology, 19(1), 17-23. https://doi.org/10.1111/j.1440-1681.1992.tb00392.x