Effects of aporphine isomers on rat prolactin.
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.
Baldessarini
R J
RJ
Consolidated Department of Psychiatry, Harvard Medical School, Boston, MA.
Campbell
A
A
Ben-Jonathan
N
N
Ellingboe
J
J
Zong
R
R
Neumeyer
J L
JL
D000818:Animals; D001058:Apomorphine / Q000031:analogs & derivatives / Q000494:pharmacology; D001060:Aporphines / Q000494:pharmacology*; D018491:Dopamine Agonists / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D008297:Male; D011388:Prolactin / Q000097:blood*; D011863:Radioimmunoassay; D051381:Rats; D017207:Rats, Sprague-Dawley; D017448:Receptors, Dopamine D2 / Q000819:agonists; D013237:Stereoisomerism
D001060:Aporphines; D018491:Dopamine Agonists; D017448:Receptors, Dopamine D2; C009074:N-n-propylnorapomorphine; C008081:11-hydroxy-N-(n-propyl)noraporphine; D011388:Prolactin; D006220:Haloperidol; D001058:Apomorphine