Literature DB >> 17612788

Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro.

R A Lahti1, C A Tamminga, A Carlsson.   

Abstract

The effect of (-)-OSU6162 on the incorporation of GTPgammaS(35) in the membranes of hD(2l)-transfected CHO cells was investigated. In the absence of dopamine the compound exerted a slight but significant stimulating action, suggesting a weak partial agonism. In the presence of dopamine, low concentrations (10 to 100 nM) enhanced the stimulating action of dopamine. This enhancing effect was reversed by higher concentrations of (-)-OSU6162 in a complex biphasic manner. The dopamine-enhancing action is proposed to be mediated by binding to an allosteric site with high affinity and the inhibitory component by a low-affinity binding to the orthosteric site of the dopamine receptor.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17612788     DOI： 10.1007/s00702-007-0784-7

Source DB:  PubMed          Journal:  J Neural Transm (Vienna)        ISSN： 0300-9564            Impact factor:   3.575


  11 in total

1.  Dopamine D2 receptor-mediated inhibition of dopaminergic neurons in mice lacking D2L receptors.

Authors:  Diego Centonze; Alessandro Usiello; Paolo Gubellini; Antonio Pisani; Emiliana Borrelli; Giorgio Bernardi; Paolo Calabresi
Journal:  Neuropsychopharmacology       Date:  2002-11       Impact factor: 7.853

2.  Prominence of the dopamine D2 short isoform in dopaminergic pathways.

Authors:  Z U Khan; L Mrzljak; A Gutierrez; A de la Calle; P S Goldman-Rakic
Journal:  Proc Natl Acad Sci U S A       Date:  1998-06-23       Impact factor: 11.205

3.  The dopamine stabilizers (S)-(-)-(3-methanesulfonyl-phenyl)-1-propyl-piperidine [(-)-OSU6162] and 4-(3-methanesulfonylphenyl)-1-propyl-piperidine (ACR16) show high in vivo D2 receptor occupancy, antipsychotic-like efficacy, and low potential for motor side effects in the rat.

Authors:  Sridhar Natesan; Kjell A Svensson; Greg E Reckless; José N Nobrega; Karen B L Barlow; Anette M Johansson; Shitij Kapur
Journal:  J Pharmacol Exp Ther       Date:  2006-04-28       Impact factor: 4.030

4.  Dopamine partial agonist action of (-)OSU6162 is consistent with dopamine hyperactivity in psychosis.

Authors:  Philip Seeman; Hong-Chang Guan
Journal:  Eur J Pharmacol       Date:  2006-11-14       Impact factor: 4.432

5.  Comparison of in vitro binding properties of a series of dopamine antagonists and agonists for cloned human dopamine D2S and D2L receptors and for D2 receptors in rat striatal and mesolimbic tissues, using [125I] 2'-iodospiperone.

Authors:  J E Leysen; W Gommeren; J Mertens; W H Luyten; P J Pauwels; M Ewert; P Seeburg
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

6.  Intrinsic activity determinations at the dopamine D2 guanine nucleotide-binding protein-coupled receptor: utilization of receptor state binding affinities.

Authors:  R A Lahti; L M Figur; M F Piercey; P L Ruppel; D L Evans
Journal:  Mol Pharmacol       Date:  1992-09       Impact factor: 4.436

7.  Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.

Authors:  A Malmberg; D M Jackson; A Eriksson; N Mohell
Journal:  Mol Pharmacol       Date:  1993-05       Impact factor: 4.436

Review 8.  Schizophrenia: from dopamine to glutamate and back.

Authors:  M L Carlsson; A Carlsson; M Nilsson
Journal:  Curr Med Chem       Date:  2004-02       Impact factor: 4.530

9.  Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.

Authors:  C Sonesson; C H Lin; L Hansson; N Waters; K Svensson; A Carlsson; M W Smith; H Wikström
Journal:  J Med Chem       Date:  1994-08-19       Impact factor: 7.446

Review 10.  A dopaminergic deficit hypothesis of schizophrenia: the path to discovery.

Authors:  Arvid Carlsson; Maria L Carlsson
Journal:  Dialogues Clin Neurosci       Date:  2006       Impact factor: 5.986
View more
  7 in total

1.  Effects of (-)-OSU6162 and ACR16 on motor activity in rats, indicating a unique mechanism of dopaminergic stabilization.

Authors:  Johan P Rung; Emilia Rung; Lisa Helgeson; Anette M Johansson; Kjell Svensson; Arvid Carlsson; Maria L Carlsson
Journal:  J Neural Transm (Vienna)       Date:  2008-03-20       Impact factor: 3.575

2.  II. In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors.

Authors:  Ethan S Burstein; Maria L Carlsson; Michelle Owens; Jian-Nong Ma; Hans H Schiffer; Arvid Carlsson; Uli Hacksell
Journal:  J Neural Transm (Vienna)       Date:  2011-08-25       Impact factor: 3.575

3.  Effects of the dopamine stabilizers (S)-(-)-OSU6162 and ACR16 on prolactin secretion in drug-naive and monoamine-depleted rats.

Authors:  Johan P Rung; Emilia Rung; Anette M Johansson; Kjell Svensson; Arvid Carlsson; Maria L Carlsson
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2011-05-02       Impact factor: 3.000

4.  I. In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors.

Authors:  Maria L Carlsson; Ethan S Burstein; Angélica Kloberg; Sarah Hansson; Arja Schedwin; Marie Nilsson; Johan P Rung; Arvid Carlsson
Journal:  J Neural Transm (Vienna)       Date:  2011-08-28       Impact factor: 3.575

5.  Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor.

Authors:  Elodie Kara; Hong Lin; Kjell Svensson; Anette M Johansson; Philip G Strange
Journal:  Br J Pharmacol       Date:  2010-11       Impact factor: 8.739

6.  The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects.

Authors:  Nelleke Tolboom; Henk W Berendse; Josee E Leysen; Maqsood Yaqub; Bart N M van Berckel; Robert C Schuit; Mirthe M Ponsen; Esther Bakker; Nikie J Hoetjes; Albert D Windhorst; Maria L Carlsson; Adriaan A Lammertsma; Arvid Carlsson
Journal:  Neuropsychopharmacology       Date:  2014-08-05       Impact factor: 7.853

7.  Effects of the monoamine stabilizer (-)OSU6162 on cognitive function in alcohol dependence.

Authors:  Lotfi Khemiri; Pia Steensland; Joar Guterstam; Örjan de Manzano; Johan Franck; Nitya Jayaram-Lindström
Journal:  Psychopharmacology (Berl)       Date:  2019-10-18       Impact factor: 4.530
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.