Benztropine (3α-Diphenylmethoxy Tropane) Analogs List of cocaine analogues

benzatropine (bzt)
difluoropine (o-620), more selective dari cocaine. anticholinergic & antihistamine.
ahn 1-055 same structure benztropine 4′,4′-bisfluorinated.
ga 103 n-phenylpropyl bis-4-fluorobenztropine.
jhw 007 n-(n-butyl)-3α-[bis(4′-fluorophenyl)methoxy]-tropane.

unlike cocaine & phenyltropanes, benztropines & gbr compounds (and, exception cocaine pharmacophore itself, allotropacocaine) among others considered atypical dat re-uptake pump ligands because stabilize dopamine transporter in inward-facing or closed-to-out conformation, contrasts considered cocaine-like affinity dat; instead keep dat stable in open-to-out conformation. means binding of many dopamine reuptake inhibitors atypical of cocaine s method of binding dat , diverges it.

difluoropine not phenyltropane belongs benzatropine family of dris. not confused diaryl -phenyltropanes.

in respects these important because share sar overlap gbr 12909 , related analogs.

sars have shown 4′,4′-difluorination excellent way boost dat activity of benztropine, , gives excellent selectivity on sert , net.

furthermore, replacing n-me with, e.g. n-phenylpropyl helps bring muscarinic activity down same dri affinity.

this remarkable considering unmodified (native) benztropine 60 times more active anticholinergic dopaminergic.

m1 receptor considerations aside, analogues of benztropine class still won t substitute cocaine, , have no propensity elevate locomotor activity.

compound 276



etybenzatropine





compound 277

inhibition @ 10 µm

deuterium labeled radio-ligand of benztropine analog jhw-007; di-para-fluoro benztropine, , hybrid between benzatropine & difluoropine (with fluorine groups in former breach difference or latter being descarbmethoxy approach identification former).

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