Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin

  title={Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin},
  author={T. B. A. Mulder and Jan B. de Vries and Durk Dijkstra and Johann W. Wiechers and Cor J. Grol and Alan S. Horn},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
SummaryThe in vitro binding of the putative dopamine autoreceptor agonist [3H]DP-7-ATN to rat striatal membrane homogenates was investigated. The maximum number of binding sites Bmax was 497.5 ± 50.2 fmol/mg protein and the affinity constant KD was 8.3 ± 1.5 nM using 10 μM (+) butaclamol to define non-specific binding. Lesion of the left medium forebrain bundle by 6-hydroxydopamine resulted in an almost complete loss of dopamine in the striatum but did not affect the binding of [3H]DP-7-ATN… 
Behavioural effects in the rat of the putative dopamine D3 receptor agonist 7-OH-DPAT: comparison with quinpirole and apomorphine
Together, the data suggest that the putative dopamine D3 agonist 7-OH-DPAT, at low doses, has depressant effects similar to those induced by low doses of the other two DA agonists.
Upregulation of (+)-7-Hydroxy-N,N-di-n-[3H]Propyl-2-Aminotetralin Binding Following Intracerebroventricular Administration of a Nitric Oxide Generator
D3 receptor density is modified following nitric oxide generation, and the density of high affinity D2 receptors identified by [3H](+)-7-OH-DPAT increases in the striatum, but decreases in the nucleus accumbens.
Characterization of binding sites for [125I]R(+)trans-7-OH-PIPAT in rat brain
[125I]R(+)trans-7-OH-PIPAT offers several unique advantages, including high specific activity and high affinity binding, which make it an excellent probe for the investigation and characterization of the distribution of dopamine D 3 receptors.


Sodium dependent [3H]cocaine binding associated with dopamine uptake sites in the rat striatum and human putamen decrease after dopaminergic denervation and in Parkinsons disease
It is concluded that [3H]cocaine may be a useful ligand to examine the dopamine transporter in the rat striatum and the human putamen and offers a new and valuable approach in the study of drug effects and neuropsychiatric diseases.
A comparison of the potencies of various dopamine receptor agonists in models for pre- and postsynaptic receptor activity
It may be concluded that N,N-dipropyl-2-amino-7-hydroxytetralin shows the largest difference in activity in the biochemical and the behavioural models, suggesting a selective presynaptic activity.
Binding characteristics of the dopamine uptake inhibitor [3H]nomifensine to striatal membranes.
S(−)DP-5,6-ADTN as an in vivo dopamine receptor ligand: Relation between displacement by dopamine agonists and their pharmacological effects
The results are discussed in view of theories on the relation between receptor occupation and pharmacological effects and it is concluded that the in vivo receptor binding method using (−)DP-5,6-ADTN is a very useful tool for such investigations.
Relationship between levels and uptake of serotonin and high affinity [3H]imipramine recognition sites in the rat brain.
The results suggest that high affinity [3H]imipramine binding in the brain is directly related to the integrity of serotonergic neurons but not to the magnitude of the uptake or the endogenous levels of the transmitter, and is not affected by damage to noradrenergic neurons or by low levels of Noradrenaline.