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OSU-6162

Chemical compound

Summary

Chemical compound

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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. 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.

References

References

  1. (July 1997). "(-)-OSU 6162 inhibits levodopa-induced dyskinesias in a monkey model of Parkinson's disease". NeuroReport.
  2. (April 1998). "Effects of the substituted (S)-3-phenylpiperidine (-)-OSU6162 on PET measurements in subhuman primates: evidence for tone-dependent normalization of striatal dopaminergic activity". Synapse.
  3. (October 1999). "Long-lasting improvement following (-)-OSU6162 in a patient with Huntington's disease". Neurology.
  4. (October 2002). "PNU-96391A (OSU6162) antagonizes the development of behavioral sensitization induced by dopamine agonists in a rat model for Parkinson's disease". Neuropharmacology.
  5. (April 2002). "Partial dopamine agonists and dopaminergic stabilizers, in the treatment of psychosis". Current Drug Targets. CNS and Neurological Disorders.
  6. (January 2006). "The substituted (S)-3-phenylpiperidine (-)-OSU6162 reduces apomorphine- and amphetamine-induced behaviour in Cebus apella monkeys". Journal of Neural Transmission.
  7. (June 2005). "The dopaminergic stabilizers (-)-OSU6162 and ACR16 reverse (+)-MK-801-induced social withdrawal in rats". Progress in Neuro-Psychopharmacology & Biological Psychiatry.
  8. (August 2006). "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.
  9. (February 2007). "Dopamine partial agonist action of (-)OSU6162 is consistent with dopamine hyperactivity in psychosis". European Journal of Pharmacology.
  10. (September 2007). "Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro". Journal of Neural Transmission.
  11. (June 2008). "Effects of (-)-OSU6162 and ACR16 on motor activity in rats, indicating a unique mechanism of dopaminergic stabilization". Journal of Neural Transmission.
  12. (June 2009). "Effects of the dopamine stabilizer, OSU-6162, on brain stimulation reward and on quinpirole-induced changes in reward and locomotion". European Neuropsychopharmacology.
  13. (February 2010). "The dopaminergic stabilizers pridopidine (ACR16) and (-)-OSU6162 display dopamine D(2) receptor antagonism and fast receptor dissociation properties". European Journal of Pharmacology.
  14. (November 2010). "Analysis of the actions of the novel dopamine receptor-directed compounds (S)-OSU6162 and ACR16 at the D2 dopamine receptor". British Journal of Pharmacology.
  15. (November 2011). "I. In vivo evidence for partial agonist effects of (-)-OSU6162 and (+)-OSU6162 on 5-HT2A serotonin receptors". Journal of Neural Transmission.
  16. (November 2011). "II. In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors". Journal of Neural Transmission.
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3-phenylpiperidines benzosulfones dopamine-agonists experimental-non-hallucinogens experimental-psychiatric-drugs non-hallucinogenic-5-ht2a-receptor-agonists propyl-compounds
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