EFFECTS OF APORPHINE ISOMERS ON RAT PROLACTIN

被引:7
作者
BALDESSARINI, RJ
CAMPBELL, A
BENJONATHAN, N
ELLINGBOE, J
ZONG, RS
NEUMEYER, JL
机构
[1] HARVARD UNIV,SCH MED,CONSOLIDATED DEPT PSYCHIAT,BOSTON,MA
[2] HARVARD UNIV,SCH MED,NEUROSCI PROGRAM,BOSTON,MA 02115
[3] MASSACHUSETTS GEN HOSP,MCLEAN DIV,MAILMAN RES CTR,BELMONT,MA
[4] MASSACHUSETTS GEN HOSP,MCLEAN DIV,ALCOHOL & ADDICT RES CTR,BELMONT,MA
[5] UNIV CINCINNATI,DEPT ANAT & CELL BIOL,CINCINNATI,OH 45267
[6] NORTHEASTERN UNIV,COLL PHARM & ALLIED HLTH PROFESS,MED CHEM SECT,BOSTON,MA 02115
[7] RES BIOCHEM INT,NATICK,MA
关键词
ANTIPSYCHOTIC; APORPHINE; DOPAMINE; PARTIAL AGONIST; PROLACTIN; RECEPTOR; STEREOISOMER;
D O I
10.1016/0304-3940(94)90098-1
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
S(+)-aporphines are partial agonists at D-2 dopamine receptors. High selectivity of anti-dopaminergic action in limbic vs. extrapyramidal 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 D-2 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.
引用
收藏
页码:269 / 271
页数:3
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