OSU-6162

From WikiMD's Wellness Encyclopedia

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.[1][2][3][4][5][6][7][8][9][10][11][12][13][14] 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.[15][16]

See also[edit | edit source]

References[edit | edit source]

  1. ↑ 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
  2. ↑ 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
  3. ↑ 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
  4. ↑ 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
  5. ↑ 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
  6. ↑ 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
  7. ↑ 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
  8. ↑ Natesan S, Svensson KA, Reckless GE, Nobrega JN, Barlow KB, Johansson AM, Kapur S. 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. Journal of Pharmacology and Experimental Therapeutics. 2006 Aug;318(2):810-8. PMID 16648369
  9. ↑ 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
  10. ↑ 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
  11. ↑ 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
  12. ↑ 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
  13. ↑ 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
  14. ↑ 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
  15. ↑ 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
  16. ↑ 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



WikiMD
Navigation: Wellness - Encyclopedia - Health topics - Disease Index‏‎ - Drugs - World Directory - Gray's Anatomy - Keto diet - Recipes

Search WikiMD

Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD

WikiMD's Wellness Encyclopedia

Let Food Be Thy Medicine
Medicine Thy Food - Hippocrates

Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates Wikipedia, licensed under CC BY SA or similar.

Retrieved from "https://wikimd.com/w/index.php?title=OSU-6162&oldid=4970147"

Contributors: Prab R. Tumpati, MD