Effect of a novel benzamide, YM-09151-2, on rat serum prolactin levels

Herbert Y. Meltzer*, Masahiko Mikuni, Miljana Simonovic, Gary A. Gudelsky

*Corresponding author for this work

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

YM-09151-2(cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide) is a new benzamide which has been reported to be an antagonist of dopamine (DA) at D1-type DA receptors. In the present study, we have examined the extent of the interaction of YM-09151-2 with D2-type DA receptors in the anterior pituitary gland of the rat. YM-09151-2 was found to be a potent antagonist of these receptors as extremely low doses of this compound produced a marked, dose-dependent elevation of serum prolactin concentrations. This benzamide was also a potent blocker 3f DA-induced inhibition of prolactin release in vitro and was very effective in displacing 3H-spiperone from bovine pituitary membranes: IC50, 1.04nM. These results are consistent with recent evidence that YM-09151-2 is also a potent antagonist of the D2-type receptors in the intermediate lobe of the rat pituitary gland.

Original languageEnglish (US)
Pages (from-to)1015-1021
Number of pages7
JournalLife Sciences
Volume32
Issue number9
DOIs
StatePublished - Feb 28 1983

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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