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OSU-6162

С Википедије, слободне енциклопедије
OSU-6162
IUPAC ime
(3S)-3-[3-(metilsulfonil)fenil]-1-propilpiperidin
Identifikatori
CAS broj156907-84-5 ДаY
ATC kodnone
PubChemCID 9795741
Hemijski podaci
FormulaC15H23NO2S
Molarna masa281,413 g/mol
  • CCCN1CCC[C@H](C1)C2=CC(=CC=C2)S(=O)(=O)C

OSU-6162 (PNU-96391) je jedinjenje koje deluje kao parcijalni agonist na dopaminskom D2 receptoru i na 5-HT2A receptoru. On deluje kao stabilizator dopamina na sličan način sa srodnim lekom pridopidinom, i ima antipsihotične, antiadiktivne i antiparkinsoniske efekte u životinjskim studijama.[1][2][3][4][5][6][7][8][9][10][11][12][13][14] Oba enantiomera pokazuju sličnu aktivnost ali imaju različite odnose efekata, pri čemu se (S) enantiomer (-)-OSU-6162 češće koristi u istraživanjima. On ima veći afinitet vezivanja za D2 ali je slabiji parcijalni agonist na 5-HT2A receptoru, dok (R) enantiomer (+)-OSU-6162 ima veću efikasnost na 5-HT2A i niži afinitet za D2 receptoru.[15][16]

Reference

[уреди | уреди извор]
  1. ^ Ekesbo, Anna; Andrén, Per E.; Gunne, Lars M.; Tedroff, Joakim (јул 1997). „(−)-OSU 6162 inhibits levodopa-induced dyskinesias in a monkey model of Parkinsonʼs disease”. NeuroReport. 8 (11): 2567—70. PMID 9261828. doi:10.1097/00001756-199707280-00029. }-
  2. ^ Tedroff, J.; Torstenson, R.; Hartvig, P.; Sonesson, C.; Waters, N.; Carlsson, A.; Neu, H.; Fasth, K.-J.; l�Ngstr�m, B. (април 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. 28 (4): 280—7. PMID 9517836. doi:10.1002/(SICI)1098-2396(199804)28:4<280::AID-SYN3>3.0.CO;2-5.  replacement character у |last9= на позицији 2 (помоћ)
  3. ^ Tedroff, J.; Ekesbo, A.; Sonesson, C.; Waters, N.; Carlsson, A. (октобар 1999). „Long-lasting improvement following (-)-OSU6162 in a patient with Huntington's disease”. Neurology. 53 (7): 1605—6. PMID 10534281. doi:10.1212/WNL.53.7.1605. 
  4. ^ Nichols, N.F; Cimini, M.G; Haas, J.V; Staton, B.A; Tedroff, J.; Svensson, K.A (октобар 2002). „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. PMID 12384167. doi:10.1016/S0028-3908(02)00144-2. 
  5. ^ Tamminga, C.; Carlsson, A. (април 2002). „Partial dopamine agonists and dopaminergic stabilizers, in the treatment of psychosis”. Current Drug Targets. CNS and Neurological Disorders. 1 (2): 141—7. PMID 12769623. doi:10.2174/1568007024606195. 
  6. ^ Brandt-Christensen, M.; Andersen, M. B.; Fink-Jensen, A.; Werge, T.; Gerlach, J. (јануар 2006). „The substituted (S)-3-phenylpiperidine (−)-OSU6162 reduces apomorphine- and amphetamine-induced behaviour in Cebus apella monkeys”. Journal of Neural Transmission. 113 (1): 11—9. PMID 15795789. doi:10.1007/s00702-005-0297-1. 
  7. ^ Rung, Johan P.; Carlsson, Arvid; Markinhuhta, Katarina Rydén; Carlsson, Maria L. (јун 2005). „The dopaminergic stabilizers (−)-OSU6162 and ACR16 reverse (+)-MK-801-induced social withdrawal in rats”. Progress in Neuropsychopharmacology and Biological Psychiatry. 29 (5): 833—9. PMID 15913873. doi:10.1016/j.pnpbp.2005.03.003. 
  8. ^ Natesan, Sridhar; Svensson, Kjell A.; Reckless, Greg E.; Nobrega, José N.; Barlow, Karen B.L.; Johansson, Anette M.; Kapur, Shitij (август 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”. Journal of Pharmacology and Experimental Therapeutics. 318 (2): 810—8. PMID 16648369. doi:10.1124/jpet.106.102905. 
  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, R. A.; Tamminga, C. A.; Carlsson, A. (септембар 2007). „Stimulating and inhibitory effects of the dopamine "stabilizer" (−)-OSU6162 on dopamine D2 receptor function in vitro”. Journal of Neural Transmission. 114 (9): 1143—6. PMID 17612788. doi:10.1007/s00702-007-0784-7. 
  11. ^ Rung, Johan P.; Rung, Emilia; Helgeson, Lisa; Johansson, Anette M.; Svensson, Kjell; Carlsson, Arvid; Carlsson, Maria L. (јун 2008). „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. PMID 18351286. doi:10.1007/s00702-008-0038-3. 
  12. ^ Benaliouad, Faïza; Kapur, Shitij; Natesan, Sridhar; Rompré, Pierre-Paul (јун 2009). „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. PMID 19269794. doi:10.1016/j.euroneuro.2009.01.014. 
  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, A. M.; Strange, P. G. (новембар 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. 161 (6): 1343—50. PMC 3000658 Слободан приступ. PMID 20804495. doi:10.1111/j.1476-5381.2010.01010.x. 
  15. ^ Carlsson, Maria L.; Burstein, Ethan S.; Kloberg, Angélica; Hansson, Sarah; Schedwin, Arja; Nilsson, Marie; Rung, Johan P.; Carlsson, Arvid (новембар 2011). „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. PMID 21874578. doi:10.1007/s00702-011-0704-8. 
  16. ^ Burstein, Ethan S.; Carlsson, Maria L.; Owens, Michelle; Ma, Jian-Nong; Schiffer, Hans H.; Carlsson, Arvid; Hacksell, Uli (новембар 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. 118 (11): 1523—33. PMID 21866391. doi:10.1007/s00702-011-0701-y. 

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