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

Herbert Y. Meltzer; Masahiko Mikuni; Miljana Simonovic; Gary A. Gudelsky

doi:10.1016/0024-3205(83)90933-5

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

Psychiatry and Behavioral Sciences

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	1015-1021
Number of pages	7
Journal	Life Sciences
Volume	32
Issue number	9
DOIs	https://doi.org/10.1016/0024-3205(83)90933-5
State	Published - Feb 28 1983

ASJC Scopus subject areas

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

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

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.",

author = "Meltzer, {Herbert Y.} and Masahiko Mikuni and Miljana Simonovic and Gudelsky, {Gary A.}",

note = "Funding Information: Supported, in part, by USPHS MH 30938, the State of Illinois Department of Mental Health and by a Pharmaceutical Manufacturers Association Foundation Grant to GAG. HYM is recipient of USPHS RCSA MH 47808.",

year = "1983",

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doi = "10.1016/0024-3205(83)90933-5",

language = "English (US)",

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T1 - Effect of a novel benzamide, YM-09151-2, on rat serum prolactin levels

AU - Meltzer, Herbert Y.

AU - Mikuni, Masahiko

AU - Simonovic, Miljana

AU - Gudelsky, Gary A.

N1 - Funding Information: Supported, in part, by USPHS MH 30938, the State of Illinois Department of Mental Health and by a Pharmaceutical Manufacturers Association Foundation Grant to GAG. HYM is recipient of USPHS RCSA MH 47808.

PY - 1983/2/28

Y1 - 1983/2/28

N2 - 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.

AB - 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.

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

Abstract

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