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Effects of aporphine isomers on rat prolactin.

Abstract
S(+)-aporphines are partial agonists at D2 dopamine receptors. High selectivity of anti-dopaminergic action in limbic vs. extrapyr amidal regions of rat brain and lack of induction of dopaminergic supersensitivity have suggested their potential as atypical antipsychotic drugs. Now, in testing for effects on circulating prolactin, a typical D2 antagonist haloperidol elevated, and potent agonist R(-)-11-hydroxy-N-propylnoraporphine lowered, serum prolactin levels in gentled male rats, while S(+)-N-propylnorapomorphine and its 11-monohydroxy analog had little or no effect, even at high doses. Lack of hyperprolactinemia adds to characteristics of S(+)-aporphines that are desirable in improved antipsychotics.
AuthorsR J Baldessarini, A Campbell, N Ben-Jonathan, J Ellingboe, R Zong, J L Neumeyer
JournalNeuroscience letters (Neurosci Lett) Vol. 176 Issue 2 Pg. 269-71 (Aug 01 1994) ISSN: 0304-3940 [Print] Ireland
PMID7830962 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Aporphines
  • Dopamine Agonists
  • Receptors, Dopamine D2
  • N-n-propylnorapomorphine
  • 11-hydroxy-N-(n-propyl)noraporphine
  • Prolactin
  • Haloperidol
  • Apomorphine
Topics
  • Animals
  • Apomorphine (analogs & derivatives, pharmacology)
  • Aporphines (pharmacology)
  • Dopamine Agonists (pharmacology)
  • Haloperidol (pharmacology)
  • Male
  • Prolactin (blood)
  • Radioimmunoassay
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 (agonists)
  • Stereoisomerism

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