2β-substitutions (including transesterification metabolite substitution cocaethylene) List of cocaine analogues

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extra methylene length 196c cocaine analogue, given in error previously; 2-methylpropyl , i.e. isobutanol.




the consideration large, bulky c2 substituents alter tropane distorting piperidine ring part of skeleton sufficiently enough impair functionality, or in said event such hamper binding, in particular @ 8-aza end ease steric strain going toward place 2-position, appear in many cases unfounded. (examples shown in collapsed/bundled table of images below)



intermediate compound #203









compound 197b displayed 1,131-fold increased selectivity in affinity on serotonin transporter, slight reductions in potency dopamine & norepinephrine transporters. whereas 197c had 469× increase @ sert, greater affinity dat cocaine & approximately equipotent net. 197b 137×, , 196c 27× less potent @ binding serotonin transporter, both had net / dat ratio made better dopaminergic cocaine.















bioisostere 2-position carbmethoxy-ester functional replacements



benzoylecgonine, i.e. compound 197e, (differing cocaine parent de-methylation of c2 carbmethoxy of carboxy) has extreme loss in potency (its approximate affinity being 195,000 nm) displayed in vitro methodologies determining binding efficacy (wherein bbb penetration not factor-in on matter in manner in vivo studies) , posited due possibly zwitterion formation.








2-[(2-methoxy-2-oxoethoxy)methyl] cocaine analogue.




[h3-n-methyl]-cocaine: reagent analogue used in radio-labeling ligand binding sites.




c2-ethyl-oso2cf2 cocaine analogue.




vinylogous 2β-position carbmethoxy-ester functional replacements


201b & 201c show significant increased potency on cocaine; whereas 201a, 201d & 201e considerably less so. infers hydrogen bond acceptor @ 2β position not of exclusive import in creation of higher binding analogues of cocaine.



[h5-phenyl]-cocaine: reagent analogue, above thumbnail of similar compound: rendered cocaine parent replacing cluster of several adjacent hydrogens (from among hydrogens comprise entire circumference common every basic molecular perimeter) deuterium, in equivalent localized spread or cluster.






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