Cocaine receptors: In vivo labeling with 3H‐(—)cocaine, 3H‐win 35,065‐2, and 3H‐win 35,428

  title={Cocaine receptors: In vivo labeling with 3H‐(—)cocaine, 3H‐win 35,065‐2, and 3H‐win 35,428},
  author={Ursula A Scheffel and John W. Boja and Michael J. Kuhar},

Rate of binding of various inhibitors at the dopamine transporter in vivo

There was no obvious correlation between rate of occupancy in this animal model and abuse liability in humans, which is consistent with the notion that other factors are critical as well.

Novel Fluorescent Ligands Enable Single-Molecule Localization Microscopy of the Dopamine Transporter.

New fluorescently labeled ligands that bind DAT with high affinity and enable single-molecule detection of the transporter are developed and can be used in direct stochastic optical reconstruction microscopy experiments permitting further analyses of DAT distribution on the nanoscale.

Structure-Activity Relationships for a series of bis(4-fluorophenyl)methyl)sulfinyl)alkyl alicyclic amines at the dopamine transporter: functionalizing the terminal nitrogen affects affinity, selectivity and metabolic stability.

Results support further investigation of 14a as a potential treatment for psychostimulant use disorders, and a series of bis(4-fluorophenyl)methyl)sulfinyl)alkyl alicyclic amines designed, synthesized and evaluated for binding affinities at DAT, as well as the serotonin transporter and sigma1 receptors.

Dopamine Transporter Dynamics of N-Substituted Benztropine Analogs with Atypical Behavioral Effects

Findings provide more detail on ligand-induced DAT conformations and indicate that aspects of DAT conformation other than “open” versus “closed” may facilitate predictions of the actions of D AT inhibitors and may promote rational design of potential treatments for psychomotor-stimulant abuse.

Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.

A series of modafinil analogues that have an atypical DAT inhibitor profile are reported, including 11b, which demonstrated high DAT affinity and selectivity without producing concomitant locomotor stimulation in mice, as compared to cocaine.

O-H⋅⋅⋅N and C-H⋅⋅⋅O hydrogen bonds control hydration of pivotal tropane alkaloids: tropinone⋅⋅⋅H(2)O complex.

The effect of monohydration in equatorial/axial isomerism of the common motif of tropane alkaloids is investigated in a supersonic expansion by using Fourier-transform microwave spectroscopy and the experimental work is supported by theoretical calculations.

Pharmacological Characterization of a Dopamine Transporter Ligand That Functions as a Cocaine Antagonist

It is suggested that JHW007 has cocaine-antagonist effects that are deviate from its DAT occupancy and that some other mechanism, possibly σ-receptor antagonist activity, may contribute to the cocaine-ANTagonist effect of JhW007 and like drugs.

Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.

In vitro competition binding assays demonstrated that compounds 9-12 have a high affinity for the DAT and are selective for theDAT compared to the serotonin and norepinephrine transporters.

N-Methyl stereochemistry in tropinone: the conformational flexibility of the tropane motif.

The intrinsic conformational and structural properties of the tropinone azabicycle have been investigated in a supersonic jet expansion using rotational spectroscopy. The spectrum revealed the



Disposition of toxic drugs and chemicals in man

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Cocaine receptors on dopamine transporters are related to self-administration of cocaine.

It is shown here that the potencies of cocaine-like drugs in self-administration studies correlate with their potencies in inhibiting [3H]mazindol binding to the dopamine transporters in the rat striatum, but not with theirPotencies in binding to a large number of other presynaptic and postsynaptic binding sites.

Mapping cocaine binding sites in human and baboon brain in vivo

The feasibility of using [11C]cocaine and PET to map binding sites for cocaine in human brain, to monitor its kinetics, and to characterize its binding mechanism by using appropriate pharmacological challenges is demonstrated.

In vivo evaluation of striatal dopamine reuptake sites using 11C‐nomifensine and positron emission tomography

Results indicate that in vivo the striatal uptake of 11C‐nomifensine, as measured with PET, involves specific binding with the dopamine reuptake sites in the brain.

Dopamine transporter: biochemistry, pharmacology and imaging.

In vivo labeling studies of the dopamine transporter have revealed the usefulness of imaging the transporter, a measure of the presence of dopaminergic nerve terminals, as a potential diagnostic tool in Parkinson's disease.