[3H]Threo‐(±)‐Methylphenidate Binding to 3,4‐Dihydroxyphenylethylamine Uptake Sites in Corpus Striatum: Correlation with the Stimulant Properties of Ritalinic Acid Esters

  title={[3H]Threo‐(±)‐Methylphenidate Binding to 3,4‐Dihydroxyphenylethylamine Uptake Sites in Corpus Striatum: Correlation with the Stimulant Properties of Ritalinic Acid Esters},
  author={Margaret M. Schweri and Phil Skolnick and Michael Francis Rafferty and Kenner C. Rice and Aaron Janowsky and Steven M Paul},
  journal={Journal of Neurochemistry},
Abstract: Saturable and stereoselective binding sites for [3H]threo‐(±)‐methylphenidate were characterized in rat brain membranes. The highest density of [3H]threo‐(±)‐ methylphenidate binding sites was found in the synapto somal fraction of corpus striatum. Scatchard analysis revealed a single class of noninteracting binding sites with an apparent dissociation constant (KD) of 235 nM and a maximum number of binding sites (Bmax) of 13.4 pmol/mg protein. Saturable, high‐affinity binding of [3H… 

Characterization of Sodium‐Dependent [3H]GBR‐12935 Binding in Brain: A Radioligand for Selective Labelling of the Dopamine Transport Complex

Data indicate that [3H]GBR‐12935 is a selective radioligand of the presynaptic dopamine transport complex in brain, with the highest concentration of binding sites being found in the corpus striatum and nucleus accumbens.

Metaphit Irreversibly Inhibits [3H]threo‐ (±)‐Methylphenidate Binding to Rat Striatal Tissue

Metaphit, a derivative of phencyclidine that contains an isothiocyanate group on the meta position of the aromatic ring, resembles its parent compound in its ability to inhibit the binding of the stimulant drug [3H]threo‐ (±)‐methylphenidate to crude synaptosomal membranes from rat Striatal tissue.

Cationic and Anionic Requirements for the Binding of 2β‐Carbomethoxy‐3β‐(4‐Fluorophenyl)[3H]tropane to the Dopamine Uptake Carrier

Abstract: The present study reports the ion dependency of 2β‐carbomethoxy‐3β‐(4‐fluorophenyl)[3H]tropane ([3H]‐ CFT) binding to the dopamine transporter in the rat striaturn. The results indicate

Carbon-11-d-threo-methylphenidate binding to dopamine transporter in baboon brain.

These results demonstrate the saturable, reversible and specific binding of [11C]d-threo-MP to the dopamine transporter on the baboon brain, suggesting that [11D-thReo- MP will be a useful PET tracer for the presynaptic dopaminergic neuron in living human brain.

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

Chiral drugs: comparison of the pharmacokinetics of [11C]d-threo and l-threo-methylphenidate in the human and baboon brain

Results indicate that pharmacological specificity of MP resides entirely in the d-threo isomer and directly show that binding of the l-isomer in human brain is mostly non-specific.

Mercuric chloride and p‐chloromercuriphenylsulfonate exert a biphasic effect on the binding of the stimulant [3H]methylphenidate to the dopamine transporter

Data suggest that the cysteine residues in the dopamine transporter molecule may play an important role in the regulation of stimulant binding to the uptake complex of rat striatal tissue.

Kinetic Analysis of the Chloride Dependence of the Neuronal Uptake of Dopamine and Effect of Anions on the Ability of Substrates to Compete with the Binding of the Dopamine Uptake Inhibitor GBR 12783

Kinetic analyses performed in different experimental conditions provide consistent results revealing that decreasing the CT concentration induced a raise in apparent Km of DA without modification of the Fmax, which is consistent with a co‐transport of Cl– and DA by the neuronal uptake system, with CT being the driving force.



(+)-Amphetamine binding to rat hypothalamus: relation to anorexic potency for phenylethylamines.

The results suggest the presence of specific receptor sites in hypothalamus that mediate the anorexic activity of amphetamine and related drugs.

[3H]mazindol binding associated with neuronal dopamine and norepinephrine uptake sites.

The association of [3H]mazindol binding sites with neuronal dopamine uptake sites in the corpus striatum is further supported by the reduction of [2-chloroethyl)-N-ethyl-2-bromobenzylamine binding sites in striatal membranes following destruction of dopaminergic neurons by 6-hydroxydopamine.

Sodium‐Sensitive Cocaine Binding to Rat Striatal Membrane: Possible Relationship to Dopamine Uptake Sites

The present results suggest that Na+–dependent cocaine binding sites are localized presynaptically on dopaminergic nerve terminals in corpus striatum, and may be related to dopamine uptake sites.

Relative Hydrolytic Rates of Certain Alkyl (b) dl-α-(2-Piperidyl)-phenylacetates

A series of alkyl esters of (b) dl-α-(2-piperidyl)-phenylacetic acid have been prepared and the kinetics of the hydroxyl ion-catalyzed hydrolysis at 80° and the hydronium ion-catalyzed hydrolysis at

Blockade by reserpine of methylphenidate-induced release of brain dopamine.

  • C. ChiuehK. Moore
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1975
Direct biochemical evidence is provided in support of the hypothesis that the central stimulant action of amphetamine and methylphenidate result from their abilities to preferentially release dopamine from "newly synthesized" and "stored" pools, respectively.