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OSU-6162
OSU-6162 (PNU-96391) is a compound which acts as a partial agonist at both dopamine D2 receptors and 5-HT2A receptors. It acts as a dopamine stabilizer in a similar manner to the closely related drug pridopidine, and has antipsychotic, anti-addictive and anti-Parkinsonian effects in animal studies.〔Ekesbo A, Andrén PE, Gunne LM, Tedroff J. (−)-OSU 6162 inhibits levodopa-induced dyskinesias in a monkey model of Parkinson's disease. ''Neuroreport''. 1997 Jul 28;8(11):2567-70. PMID 9261828〕〔Tedroff J, Torstenson R, Hartvig P, Sonesson C, Waters N, Carlsson A, Neu H, Fasth KJ, Långström B. Effects of the substituted (S)-3-phenylpiperidine (−)-OSU6162 on PET measurements in subhuman primates: evidence for tone-dependent normalization of striatal dopaminergic activity. ''Synapse''. 1998 Apr;28(4):280-7. PMID 9517836〕〔Tedroff J, Ekesbo A, Sonesson C, Waters N, Carlsson A. Long-lasting improvement following (−)-OSU6162 in a patient with Huntington's disease. ''Neurology''. 1999 Oct 22;53(7):1605-6. PMID 10534281〕〔Nichols NF, Cimini MG, Haas JV, Staton BA, Tedroff J, Svensson KA. PNU-96391A (OSU6162) antagonizes the development of behavioral sensitization induced by dopamine agonists in a rat model for Parkinson's disease. ''Neuropharmacology''. 2002 Oct;43(5):817-24. PMID 12384167〕〔Tamminga CA, Carlsson A. Partial dopamine agonists and dopaminergic stabilizers, in the treatment of psychosis. ''Current Drug Targets. CNS and Neurological Disorders''. 2002 Apr;1(2):141-7. PMID 12769623〕〔Brandt-Christensen M, Andersen MB, Fink-Jensen A, Werge T, Gerlach J. The substituted (S)-3-phenylpiperidine (−)-OSU6162 reduces apomorphine- and amphetamine-induced behaviour in Cebus apella monkeys. ''Journal of Neural Transmission''. 2006 Jan;113(1):11-9. PMID 15795789〕〔Rung JP, Carlsson A, Markinhuhta KR, Carlsson ML. The dopaminergic stabilizers (−)-OSU6162 and ACR16 reverse (+)-MK-801-induced social withdrawal in rats. ''Progress in Neuropsychopharmacology and Biological Psychiatry''. 2005 Jun;29(5):833-9. PMID 15913873〕〔Natesan S, Svensson KA, Reckless GE, Nobrega JN, Barlow KB, Johansson AM, Kapur S. The dopamine stabilizers (S)-(−)-(3-methanesulfonyl-phenyl)-1-propyl-piperidine () 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. ''Journal of Pharmacology and Experimental Therapeutics''. 2006 Aug;318(2):810-8. PMID 16648369〕〔Seeman P, Guan HC. Dopamine partial agonist action of (-)OSU6162 is consistent with dopamine hyperactivity in psychosis. ''European Journal of Pharmacology''. 2007 Feb 28;557(2-3):151-3. PMID 17157291〕〔Lahti RA, Tamminga CA, Carlsson A. Stimulating and inhibitory effects of the dopamine "stabilizer" (−)-OSU6162 on dopamine D2 receptor function in vitro. ''Journal of Neural Transmission''. 2007 Sep;114(9):1143-6. PMID 17612788〕〔Rung JP, Rung E, Helgeson L, Johansson AM, Svensson K, Carlsson A, Carlsson ML. Effects of (−)-OSU6162 and ACR16 on motor activity in rats, indicating a unique mechanism of dopaminergic stabilization. ''Journal of Neural Transmission''. 2008 Jun;115(6):899-908. PMID 18351286〕〔Benaliouad F, Kapur S, Natesan S, Rompré PP. Effects of the dopamine stabilizer, OSU-6162, on brain stimulation reward and on quinpirole-induced changes in reward and locomotion. ''European Neuropsychopharmacology''. 2009 Jun;19(6):416-30. PMID 19269794〕〔Dyhring T, Nielsen EØ, Sonesson C, Pettersson F, Karlsson J, Svensson P, Christophersen P, Waters N. The dopaminergic stabilizers pridopidine (ACR16) and (−)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties. ''European Journal of Pharmacology''. 2010 Feb 25;628(1-3):19-26. PMID 19919834〕〔Kara E, Lin H, Svensson K, Johansson AM, Strange PG. Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor. ''British Journal of Pharmacology''. 2010 Nov;161(6):1343-50. DOI 10.1111/j.1476-5381.2010.01010.x. PMID 20804495〕 Both enantiomers show similar activity but with different ratios of effects, with the (S) enantiomer (–)-OSU-6162 that is more commonly used in research, having higher binding affinity to D2 but is a weaker partial agonist at 5-HT2A, while the (R) enantiomer (+)-OSU-6162 has higher efficacy at 5-HT2A but lower D2 affinity.〔Carlsson ML, Burstein ES, Kloberg A, Hansson S, Schedwin A, Nilsson M, Rung JP, Carlsson A. I. In vivo evidence for partial agonist effects of (−)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors. ''Journal of Neural Transmission''. 2011 Nov;118(11):1511-22. PMID 21874578〕〔Burstein ES, Carlsson ML, Owens M, Ma JN, Schiffer HH, Carlsson A, Hacksell U. II. In vitro evidence that (−)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors. ''Journal of Neural Transmission''. 2011 Nov;118(11):1523-33. PMID 21866391〕
==See also==
* PF-219,061
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