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 language | English |
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Pages (from-to) | 17-23 |
Number of pages | 7 |
Journal | Clinical and Experimental Pharmacology and Physiology |
Volume | 19 |
Issue number | 1 |
DOIs | |
Publication status | Published - 1 Jan 1992 |
Keywords
- analgesics
- peripherally acting drugs
- S‐HT antagonists