Molecular features of the prazosin molecule required for activation of Transport-P.
Closely related structural analogues of prazosin have been synthesised and tested for inhibition and activation of Transport-P in order to identify the structural features of the prazosin molecule that appear to be necessary for activation of Transport-P. So far, all the compounds tested are less active than prazosin. It is shown that the structure of prazosin appears to be very specific for the activation. Only quinazolines have been found to activate, and the presence of the 6,7-dimethoxy and 4-amino groups appears to be critically important.
da Silva
Joaquim Fernando Mendes
JF
Department of Chemistry, Christopher Ingold Laboratories, University College London, 20 Gordon Street, London WC1H 0AJ, UK.
Walters
Marcus
M
Al-Damluji
Saad
S
Ganellin
C Robin
CR
D000959:Antihypertensive Agents / Q000737:chemistry / Q000494:pharmacology; D001693:Biological Transport, Active / Q000502:physiology*; D002478:Cells, Cultured; D015394:Molecular Structure; D009474:Neurons / Q000378:metabolism*; D011224:Prazosin / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000959:Antihypertensive Agents; D011224:Prazosin