Comparative properties of the dopamine transport complex in dog and rodent brain: striatal [3H]GBR12935 binding and [3H]dopamine uptake

Sharif, N.A.; Nunes, J. L.; Michel, Agnès; Whiting, Roger L.

doi:10.1016/0197-0186(89)90140-x

Cited by 13 publications

(6 citation statements)

References 20 publications

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“…The saturation experiments showed that the [3H]GBR-12935 binding to rat striatum was saturable and of high affinity within the nanomolar range, in agreement with other studies of rat striatum [6,8,13] …”

Section: Discussionsupporting

confidence: 75%

[<sup>3</sup>H]GBR-12935 Binding to Dopamine Uptake Sites in Rat Striatum

et al. 1990

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The binding of the selective dopamine uptake inhibitor [³H]GBR-12935 to rat striatum was studied. Competition by mazindol and dopamine against [³H]GBR-12935 binding revealed monophasic binding curves. The addition of 100 μM dopamine to the mazindol competition inhibited only 80% of the binding, indicating more than one [³H]GBR-12935 binding site in rat striatum. When a binding fraction that could be discriminated by 1 μM mazindol or 1 mM dopamine was defined as specific binding, a single site binding model was obtained. The [³H]GBR-12935 binding was of protein nature, since it was abolished after protease treatment. Drug inhibition studies with the addition of low concentrations of mazindol and dopamine resulted in alterations in apparent K_d values only, suggesting competitive inhibition by these compounds against [³H]GBR-12935 binding. It is concluded that the [³H]GBR-12935 binding to rat striatum discriminated by 1 μM mazindol reflects binding to the substrate recognition site for the dopamine uptake.

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Section: Discussionsupporting

confidence: 75%

[<sup>3</sup>H]GBR-12935 Binding to Dopamine Uptake Sites in Rat Striatum

et al. 1990

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“…While the presence of DAT in the nasal respiratory mucosa, a non-neuronal tissue, was somewhat unexpected, other investigators have also reported the presence of DAT outside of the CNS (Mezey et al, 1996(Mezey et al, , 1999. These sites have included the epithelial cells and the submucosal vasculature (only the veins but not the arteries) of the stomach (Mezey et al, 1999) and in the pancreatic ducts and glandular pancreatic tissue (Mezey et al, 1996) and in the kidneys (Sharif et al, 1989;Surratt et al, 1994).…”

Section: Discussionmentioning

confidence: 97%

“…Since the nasal respiratory mucosa does not contain olfactory neurons, the presence of DAT in this tissue was also investigated. DAT expression has been reported in other nonneuronal tissues including regions of the gastrointestinal system and the kidneys (Sharif et al, 1989;Surratt et al, 1994;Mezey et al, 1996Mezey et al, , 1999, and the comparison of the olfactory and respiratory mucosa with respect to the role of DAT expression, location and role in dopamine transport was an important aim of these studies.…”

Section: Introductionmentioning

confidence: 97%

Role of dopamine transporter (DAT) in dopamine transport across the nasal mucosa

et al. 2006

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“…& Although the binding kinetics (affinity and capacity) of the striatal dopamine transport complex differed in the dog, rat, guinea pig, and mouse, the rank order of binding inhibitors was the same across all four animal species (98).…”

Section: Blood-cns Partitioning: Passive Versus Active Transportmentioning

confidence: 99%

Factors Influencing the Use and Interpretation of Animal Models in the Development of Parenteral Drug Delivery Systems

Martinez

2011

AAPS J

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Abstract. Depending upon the drug and drug delivery platform, species-specific physiological differences can lead to errors in the interspecies extrapolation of drug performance. This manuscript provides an overview of the species-specific physiological variables that can influence the performance of parenteral dosage forms such as in situ forming delivery systems, nanoparticles, microspheres, liposomes, targeted delivery systems, lipophilic solutions, and aqueous suspensions. Also discussed are those factors that can influence the partitioning of therapeutic compounds into tumors, the central nervous system and the lymphatics. Understanding interspecies differences in the movement and absorption of molecules is important to the interpretation of data generated through the use of animal models when studying parenteral drug delivery.

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Comparative properties of the dopamine transport complex in dog and rodent brain: striatal [3H]GBR12935 binding and [3H]dopamine uptake

Cited by 13 publications

References 20 publications

[<sup>3</sup>H]GBR-12935 Binding to Dopamine Uptake Sites in Rat Striatum

[<sup>3</sup>H]GBR-12935 Binding to Dopamine Uptake Sites in Rat Striatum

Role of dopamine transporter (DAT) in dopamine transport across the nasal mucosa

Factors Influencing the Use and Interpretation of Animal Models in the Development of Parenteral Drug Delivery Systems

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