Chemistry:OSU-6162

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Short description: Chemical compound
OSU-6162
OSU-6162.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC15H23NO2S
Molar mass281.41 g·mol−1
3D model (JSmol)

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

References

  1. ↑ "(-)-OSU 6162 inhibits levodopa-induced dyskinesias in a monkey model of Parkinson's disease". NeuroReport 8 (11): 2567–70. July 1997. doi:10.1097/00001756-199707280-00029. PMID 9261828. 
  2. ↑ "Effects of the substituted (S)-3-phenylpiperidine (-)-OSU6162 on PET measurements in subhuman primates: evidence for tone-dependent normalization of striatal dopaminergic activity". Synapse 28 (4): 280–7. April 1998. doi:10.1002/(SICI)1098-2396(199804)28:4<280::AID-SYN3>3.0.CO;2-5. PMID 9517836. 
  3. ↑ "Long-lasting improvement following (-)-OSU6162 in a patient with Huntington's disease". Neurology 53 (7): 1605–6. October 1999. doi:10.1212/wnl.53.7.1605. PMID 10534281. 
  4. ↑ "PNU-96391A (OSU6162) antagonizes the development of behavioral sensitization induced by dopamine agonists in a rat model for Parkinson's disease". Neuropharmacology 43 (5): 817–24. October 2002. doi:10.1016/s0028-3908(02)00144-2. PMID 12384167. 
  5. ↑ "Partial dopamine agonists and dopaminergic stabilizers, in the treatment of psychosis". Current Drug Targets. CNS and Neurological Disorders 1 (2): 141–7. April 2002. doi:10.2174/1568007024606195. PMID 12769623. 
  6. ↑ "The substituted (S)-3-phenylpiperidine (-)-OSU6162 reduces apomorphine- and amphetamine-induced behaviour in Cebus apella monkeys". Journal of Neural Transmission 113 (1): 11–9. January 2006. doi:10.1007/s00702-005-0297-1. PMID 15795789. 
  7. ↑ "The dopaminergic stabilizers (-)-OSU6162 and ACR16 reverse (+)-MK-801-induced social withdrawal in rats". Progress in Neuro-Psychopharmacology & Biological Psychiatry 29 (5): 833–9. June 2005. doi:10.1016/j.pnpbp.2005.03.003. PMID 15913873. 
  8. ↑ "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". The Journal of Pharmacology and Experimental Therapeutics 318 (2): 810–8. August 2006. doi:10.1124/jpet.106.102905. PMID 16648369. 
  9. ↑ "Dopamine partial agonist action of (-)OSU6162 is consistent with dopamine hyperactivity in psychosis". European Journal of Pharmacology 557 (2–3): 151–3. February 2007. doi:10.1016/j.ejphar.2006.11.016. PMID 17157291. 
  10. ↑ "Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro". Journal of Neural Transmission 114 (9): 1143–6. September 2007. doi:10.1007/s00702-007-0784-7. PMID 17612788. 
  11. ↑ "Effects of (-)-OSU6162 and ACR16 on motor activity in rats, indicating a unique mechanism of dopaminergic stabilization". Journal of Neural Transmission 115 (6): 899–908. June 2008. doi:10.1007/s00702-008-0038-3. PMID 18351286. 
  12. ↑ "Effects of the dopamine stabilizer, OSU-6162, on brain stimulation reward and on quinpirole-induced changes in reward and locomotion". European Neuropsychopharmacology 19 (6): 416–30. June 2009. doi:10.1016/j.euroneuro.2009.01.014. PMID 19269794. 
  13. ↑ "The dopaminergic stabilizers pridopidine (ACR16) and (-)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties". European Journal of Pharmacology 628 (1–3): 19–26. February 2010. doi:10.1016/j.ejphar.2009.11.025. PMID 19919834. 
  14. ↑ "Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor". British Journal of Pharmacology 161 (6): 1343–50. November 2010. doi:10.1111/j.1476-5381.2010.01010.x. PMID 20804495. 
  15. ↑ "I. In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors". Journal of Neural Transmission 118 (11): 1511–22. November 2011. doi:10.1007/s00702-011-0704-8. PMID 21874578. 
  16. ↑ "II. In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors". Journal of Neural Transmission 118 (11): 1523–33. November 2011. doi:10.1007/s00702-011-0701-y. PMID 21866391. 



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