Literature DB >> 6128419

Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.

L Florvall, S O Ogren.   

Abstract

A series of some novel N-(l-ethyl-2-pyrrolidinylmethyl)benzamides was synthesized and tested for dopamine receptor blockade in vivo by the ability to block the apomorphine syndrome in the rat. Several compounds were considerably more potent than sulpiride as dopamine receptor blockers and displayed low liability to induce extrapyramidal side effects (catalepsy) in the rat. The blockade of dopamine receptor activity in vivo was mainly confined to the levorotatory isomers having the S absolute configuration. The structure-activity relationships are discussed.

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Year:  1982        PMID： 6128419     DOI： 10.1021/jm00353a003

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

1.  Pharmacokinetics and effects on prolactin of remoxipride in patients with tardive dyskinesia.

Authors:  E Widerlöv; U Andersson; C von Bahr; M I Nilsson
Journal:  Psychopharmacology (Berl)       Date:  1991       Impact factor: 4.530

Review 2.  A review of the discovery, pharmacological characterization, and behavioral effects of the dopamine D2-like receptor antagonist eticlopride.

Authors:  Jennifer L Martelle; Michael A Nader
Journal:  CNS Neurosci Ther       Date:  2008       Impact factor: 5.243

3.  BRL 20596, a novel anilide with central dopamine antagonist activity.

Authors:  W Campbell; M S Clark; P J Mitchell; P L Needham; J M Semple
Journal:  Psychopharmacology (Berl)       Date:  1986       Impact factor: 4.530

Review 4.  Biotransformation of post-clozapine antipsychotics: pharmacological implications.

Authors:  S Caccia
Journal:  Clin Pharmacokinet       Date:  2000-05       Impact factor: 6.447

5.  An open study of remoxipride, a benzamide derivative, in schizophrenia.

Authors:  L Lindström; G Besev; G Stening; E Widerlöv
Journal:  Psychopharmacology (Berl)       Date:  1985       Impact factor: 4.530

Review 6.  D2-receptor imaging with [123I]IBZM and single photon emission tomography in psychiatry: a survey of current status.

Authors:  R Schlösser; S Schlegel
Journal:  J Neural Transm Gen Sect       Date:  1995

7.  The effect of selective 5-hydroxytryptamine uptake inhibitors on 5-methoxy-N,N-dimethyltryptamine-induced ejaculation in the rat.

Authors:  L Rényi
Journal:  Br J Pharmacol       Date:  1986-04       Impact factor: 8.739

8.  In vivo labelling of rat brain dopamine D-2 receptors. Stereoselective blockade by the D-2 antagonist raclopride and its enantiomer of 3H-spiperone, 3H-N,N-propylnorapomorphine and 3H-raclopride binding in the rat brain.

Authors:  C Köhler; G Karlsson-Boethius
Journal:  J Neural Transm       Date:  1988       Impact factor: 3.575

9.  Crystal structure of 2-pentyl-oxybenzamide.

Authors:  Bernhard Bugenhagen; Yosef Al Jasem; Thies Thiemann
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-09-20
  9 in total

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