Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 15, Pages 7254-7263Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.06.037
Keywords
Transport-P; prazosin; peptidergic neurones; quinazoline; furan; antidepressant; amine uptake
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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. (C) 2008 Elsevier Ltd. All rights reserved.
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