User:Nuklear
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Pages Created: Ohmefentanyl (OMF) and Phenyltropane (PT). In the pipeline: Nocaine. Also see SNDRI
- Cocaine is a tropane alkaloid native to the leaves of the SAm plant Erythroxylum coca, a powerfully addicting psychostimulant reinforcer, widely abused recreationally for this purpose. Other naturally occurring tropane alkaloids include atropine and scopolamine, muscarinic AChR antagonists with radically different pharmacology to cocaine and members of the unrelated Solanaceae family, which includes alkaloids such as nicotine and capsaicin. BZ is a popular nonlethal incapacitating agent among the military, a man-made muscarinic that can be used in armed combat scenarios to wipeout the enemy. It is not harmful enough to secure a fatality, whereas deadly nightshade is more insidious. Epibatidine though, is outright lethal — and extremely popular in the military for this exact reason.[1]
The N-(γ-fluoropropyl) analogue of 2-carboisopropoxy-β-CIT is more potent than the corresponding N-methyl analogue;
"...the N-fluoropropyl-2β-carboisopropyloxy analogue of β-CIT (83a) was the most DAT selective agent over both NET (8300-fold) and 5-HTT (41-fold). It was even more potent than β-CIT. This selectivity and potency appeared to be due to the 2β-carboisopropyloxy group and not essentially due to the N-fluoropropyl group (cf. 83a vs 84a). Nevertheless, the C2 fluoropropyl group did contribute to a higher binding potency (cf. 83a vs 83b; 84a vs 84b)."
I just thought N-alkyl derivatives were worth a mention in a phenyltropanes SAR page as its another direction that could be pursued. I've got another ref somewhere where they put an SO2CF3 group onto the tropane nitrogen and that increased potency also, my point is just that there are alternatives to N-methyl that can be used!
Meodipt 11:08, 4 April 2007 (UTC)
