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Binding of bromine-substituted analogs of methylphenidate to monoamine transporters.

Abstract：

:We synthesized the o-, m- and p-bromo derivatives of dl-threo-methylphenidate from the corresponding bromophenylacetonitriles by modification of the literature synthesis of methylphenidate (Panizzon, Helv. Chim. Acta 1944, 27, 1748). In in vitro binding assays all three dl-threo bromo compounds had higher affinities than methylphenidate for dopamine transporter sites labeled with [3H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane ([3H]WIN 35,428; IC50 = 13, 4, 20 and 82 nM for o-, m-, and p-bromo compounds, and unsubstituted methylphenidate, respectively). They also bound more strongly than methylphenidate to norepinephrine reuptake sites labeled with [3H]nisoxetine (IC50 = 32, 20, 31 and 440 nM, respectively), but were weak ligands (IC50 > or = 1 microM) at the serotonin transporter labeled with [3H]paroxetine. In addition, the bromine substituted derivatives demonstrated similar activity to methylphenidate in vivo in rodents in terms of inhibition of heart uptake of [3H](-)-norepinephrine, elevation of striatal extracellular dopamine, and stimulation of locomotor activity.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Pan D,Gatley SJ,Dewey SL,Chen R,Alexoff DA,Ding YS,Fowler JS

doi

10.1016/0014-2999(94)00460-9

subject

Has Abstract

pub_date

1994-10-24 00:00:00

pages

177-82

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(94)00460-9

journal_volume

264

pub_type

杂志文章

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