Behavioral effects of (−)10, 11-methylenedioxy-n-n-propylnoraporphined, an orally effective long-acting agent active at central dopamine receptors, and analogous aporphines

@article{Campbell1982BehavioralEO,
  title={Behavioral effects of (−)10, 11-methylenedioxy-n-n-propylnoraporphined, an orally effective long-acting agent active at central dopamine receptors, and analogous aporphines},
  author={Alexander Campbell and Ross J. Baldessarini and Vishnu Ji Ram and John L Neumeyer},
  journal={Neuropharmacology},
  year={1982},
  volume={21},
  pages={953-961}
}
Behavioral effects of apomorphine isomers in the rat: Selective locomotor-inhibitory effects of S(+)N-n-propylnorapomorphine
TLDR
The results suggest that S(+)NPA or its congeners and analogs may have selective antidopaminergic actions in limbic rather than striatal areas of mammalian brain.
Prolonged antidopaminergic actions of single doses of butyrophenones in the rat
TLDR
The results indicate that some neuroleptics may have very prolonged activity or retention in tissue at sites of action, even after moderate, single doses.
Comparative assessment of dopamine agonist aporphines as anticonvulsants in two models of reflex epilepsy
TLDR
All the compounds (including norapomorphine) significantly lowered rectal temperature, although the time course of this effect was often longer than that of protection against audiogenic seizures.
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The synthesis of racemic 10-hydroxyaporphine [(+/-)-2a] and 10-hydroxy-N-n-propylnoraporphine [(+/)-2b] is described. The method involved a Reissert alkylation-Pschorr cyclization route. The
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TLDR
The present studies confirm that the flexible benzylisoquinolines 4 and 5 do not adopt the active dopamine conformation and that the rigid aporphines, preferably containing hydroxyl functions at the 10 or 11 positions, are of greater importance in eliciting potent dopamine agonist activity.
A new dopaminergic prodrug
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An improved, simplified synthesis of ADTN is developed consisting of four steps and it is described how the passage of the drug into the brain is effected, throwing new light on the in vivo action of this drug.
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