PMID: 6112770Jan 1, 1981Paper

Neuroleptic properties of cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-methylaminobenzamide (YM-09151-2) with selective antidopaminergic activity

Psychopharmacology
S UsudaH Maeno

Abstract

A new benzamide, cis-N-(1-benzyl-2-methylpyrrolidin - 3 - yl) - 5 - chloro - 2 - methoxy - 4 - methylaminobenzamide (YM-09151-2) exhibited more potent and longer-lasting inhibitory effects on apomorphine-induced behaviours (stereotyped behaviour, emesis and hypothermia), and methamphetamine-induced stereotyped behaviour, conditioned avoidance response and open field behaviour, conditioned avoidance response and open field behaviour than either structurally similar benzamides (YM-0850 and sulpiride) or classical neuroleptics [chlorpromazine (CPZ) and haloperidol(HPD)]. Such inhibitory effects of YM-09151-2 relative to cataleptogenicity were greater than those of CPz and HPD. In contrast, sulpiride elicited few of the neuroleptic effects described above. YM-09151-2, a potent inhibitor for dopamine-sensitive adenylate cyclase (Ki: 3.0 nM) reduced, in a selective manner, the binding of [3H]dopamine to the dopamine D1 receptor (Ki:4.8 nm) associated with adenylate cyclase rather than to the dopamine D2 receptor (Ki: 0.98 microM) independent of adenylate cyclase. Sulpiride, on the contrary, inhibited only the binding to the dopamine D2 receptor, CPZ and HPD antagonized [3H]dopamine nonselectively at the two distinct dopaminergic rece...Continue Reading

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Citations

Jan 1, 1986·Psychopharmacology·W CampbellJ M Semple
Mar 19, 1982·Molecular and Cellular Biochemistry·H Maeno
Jun 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·H B NiznikP Seeman
Jan 1, 1987·Journal of Neural Transmission·R MarksteinP Gull
Jun 16, 1982·European Journal of Pharmacology·C W GreweJ W Kebabian
Oct 1, 1989·Pharmacology, Biochemistry, and Behavior·S ShibanokiK Ishikawa
May 1, 1997·Pharmacology, Biochemistry, and Behavior·M YamamotoM Suzuki
Jan 1, 1997·Brain Research Bulletin·P L Marzella, D Copolov
Jan 19, 1999·FEBS Letters·P ZawarynskiS R George
Jan 1, 1984·Acta Psychiatrica Scandinavica. Supplementum·P Jenner, C D Marsden
Jun 1, 1983·The Journal of Pharmacy and Pharmacology·S FlemingerC D Marsden
Jun 1, 1988·The Journal of Pharmacy and Pharmacology·J K ChiversC D Marsden
Jan 1, 1986·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S HiguchiS Kawamura
Mar 1, 1991·Veterinary Pathology·R H Cardy
Feb 28, 1983·Life Sciences·H Y MeltzerG A Gudelsky

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