Literature DB >> 3927002

Novel dopamine receptor agonists and antagonists with preferential action on autoreceptors.

A M Johansson, L E Arvidsson, U Hacksell, J L Nilsson, K Svensson, S Hjorth, D Clark, A Carlsson, D Sanchez, B Andersson.   

Abstract

The enantiomers of cis-5-hydroxy-1-methyl-2-(di-n-propylamino)tetralin and its methyl ether have been synthesized. The compounds were tested for central dopamine (DA) receptor activity, by using biochemical and behavioral tests in rats. The (1R,2S)-(-) enantiomers of 1 and 2 are characterized as centrally acting DA-receptor agonists while the corresponding (1S,2R)-(+) enantiomers are characterized as centrally acting DA-receptor antagonists. Compounds (+)-1 and (+)-2 differ from classical neuroleptics in being able to increase DA synthesis rate in a wide dose range without reducing locomotor activity, suggesting a pronounced selectivity for DA autoreceptors. Also the (-) enantiomers seem to act preferentially on DA autoreceptors.

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Year:  1985        PMID： 3927002     DOI： 10.1021/jm00146a012

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


  6 in total

1.  (+)-UH 232 and (+)-UH 242: novel stereoselective dopamine receptor antagonists with preferential action on autoreceptors.

Authors:  K Svensson; S Hjorth; D Clark; A Carlsson; H Wikström; B Andersson; D Sanchez; A M Johansson; L E Arvidsson; U Hacksell
Journal:  J Neural Transm       Date:  1986       Impact factor: 3.575

2.  The dopamine D3-receptor: a postsynaptic receptor inhibitory on rat locomotor activity.

Authors:  N Waters; K Svensson; S R Haadsma-Svensson; M W Smith; A Carlsson
Journal:  J Neural Transm Gen Sect       Date:  1993

3.  Central dopaminergic properties of HW-165 and its enantiomers; trans-octahydrobenzo(f)quinoline congeners of 3-PPP.

Authors:  S Hjorth; K Svensson; A Carlsson; H Wikström; B Andersson
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-07       Impact factor: 3.000

4.  (+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential dopamine autoreceptor antagonists.

Authors:  K Svensson; A M Johansson; T Magnusson; A Carlsson
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-11       Impact factor: 3.000

5.  A homologous series of N-alkylated cis-(+)-(1 S, 2 R)-5-methoxy-1-methyl-2-aminotetralins: central dopamine receptor antagonists showing profiles ranging from classical antagonism to selectivity for autoreceptors.

Authors:  K Svensson; A Carlsson; A M Johansson; L E Arvidsson; J L Nilsson
Journal:  J Neural Transm       Date:  1986       Impact factor: 3.575

6.  Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin.

Authors:  T B Mulder; J B de Vries; D Dijkstra; J W Wiechers; C J Grol; A S Horn
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-11       Impact factor: 3.000
  6 in total

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