CHEMICAL DESIGN OF PERIPHERALLY ACTING COMPOUNDS
- 1 January 1992
- journal article
- Published by Wiley in Clinical and Experimental Pharmacology and Physiology
- Vol. 19 (1) , 17-23
- https://doi.org/10.1111/j.1440-1681.1992.tb00392.x
Abstract
SUMMARY: 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‐HT2antagonists. 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‐HT2pharmacophore.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.Keywords
This publication has 7 references indexed in Scilit:
- PHARMACOLOGICAL EVALUATION OF TWO NOVEL ANALOGUES OF MIANSERIN: 2-N-CARBOXAMIDINONORMIANSERIN(FCC5) AND 2-N-CARBOXAMIDONORMIANSERIN (FCC13)Clinical and Experimental Pharmacology and Physiology, 1992
- Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamineJournal of Medicinal Chemistry, 1989
- New methods in computer-aided drug designAccounts of Chemical Research, 1987
- Computer-Aided Drug DesignAnnual Review of Pharmacology and Toxicology, 1987
- Mianserin: a decade of scientific development.British Journal of Clinical Pharmacology, 1978
- Monitoring digoxin therapy: III. How useful are the nomograms?Published by Wiley ,1978
- The Distribution and Excretion by Cats of A New Hypotensive Drug, N-Benzyl-N′N″-DimethylguanidineJournal of Pharmacy and Pharmacology, 1962