1. Dear Drugs-Forum readers: We are a small non-profit that runs one of the most read drug information & addiction help websites in the world. We serve over 4 million readers per month, and have costs like all popular websites: servers, hosting, licenses and software. To protect our independence we do not run ads. We take no government funds. We run on donations which average $25. If everyone reading this would donate $5 then this fund raiser would be done in an hour. If Drugs-Forum is useful to you, take one minute to keep it online another year by donating whatever you can today. Donations are currently not sufficient to pay our bills and keep the site up. Your help is most welcome. Thank you.
    PLEASE HELP

Dopamine Uptake Inhibitors Possessing Low Binding Affinity to the Dopamine

Dopamine Uptake Inhibitors Possessing Low Binding Affinity to the Dopamine

  1. fnord
    A series of 6R- and 6 -substituted benztropines were synthesized. A marked enantioselectivity was observed for the 6 -methoxylated benztropines, the (1R)-isomers being more potent than the corresponding (1S) compounds. The racemic 6R-methoxy-3-(4′,4′′-difluorodiphenylmethoxy)- tropane (5g) was the most potent compound. It has been found that modifications at the 6-position of benztropine might reduce the DAT binding affinity, maintaining otherwise a significant dopamine uptake inhibitory activity. A reinvestigation of the absolute configuration of 6 -methoxytropinone proved the 6R configuration for the (+)-enantiomer.