Sarizotan

Sarizotan
Systematic (IUPAC) name
	1-[(2R)-3,4-dihydro-2H-chromen-2-yl]-N-([5-(4-fluorophenyl)pyridin-3-yl]methyl)methanamine
Clinical data
Pregnancy cat.	?
Legal status	Uncontrolled
Routes	Oral
Identifiers
CAS number	177975-08-5
ATC code	None
PubChem	CID 6918388
ChemSpider	2319847
UNII	467LU0UCUW
Chemical data
Formula	C22H21FN2O
Mol. mass	348.413 g/mol
SMILES	eMolecules & PubChem

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Sarizotan (EMD-128,130) is a selective 5-HT_1A receptor agonist and D₂ receptor antagonist,^[1] which has antipsychotic effects,^[2]^[3] and has also shown efficacy in reducing dyskinesias resulting from long-term anti-Parkinsonian treatment with levodopa.^[4]^[5]^[6]^[7]

[edit] See also

[edit] References

^ Rabiner, E. A.; Gunn, R. N.; Wilkins, M. R.; Sedman, E.; Grasby, P. M. (2002). "Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with 11CWAY-100635 and 11Craclopride". Journal of psychopharmacology (Oxford, England) 16 (3): 195–199. doi:10.1177/026988110201600301. PMID 12236624. edit
^ Assié, M.; Ravailhe, V.; Faucillon, V.; Newman-Tancredi, A. (2005). "Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain". The Journal of pharmacology and experimental therapeutics 315 (1): 265–272. doi:10.1124/jpet.105.087163. PMID 15987834. edit
^ Auclair, A.; Galinier, A.; Besnard, J.; Newman-Tancredi, A.; Depoortère, R. (2007). "Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats". Psychopharmacology 193 (1): 45–54. doi:10.1007/s00213-007-0762-7. PMID 17393144. edit
^ Bibbiani, F.; Oh, J. D.; Chase, T. N. (2001). "Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models". Neurology 57 (10): 1829–1834. PMID 11723272. edit
^ Bartoszyk, G.; Van Amsterdam, C.; Greiner, H.; Rautenberg, W.; Russ, H.; Seyfried, C. (2004). "Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile". Journal of neural transmission (Vienna, Austria : 1996) 111 (2): 113–126. doi:10.1007/s00702-003-0094-7. PMID 14767715. edit
^ Bara-Jimenez, W.; Bibbiani, F.; Morris, M.; Dimitrova, T.; Sherzai, A.; Mouradian, M.; Chase, T. (2005). "Effects of serotonin 5-HT1A agonist in advanced Parkinson's disease". Movement disorders : official journal of the Movement Disorder Society 20 (8): 932–936. doi:10.1002/mds.20370. PMID 15791634. edit
^ Grégoire, L.; Samadi, P.; Graham, J.; Bédard, P.; Bartoszyk, G.; Di Paolo, T. (2009). "Low doses of sarizotan reduce dyskinesias and maintain antiparkinsonian efficacy of L-Dopa in parkinsonian monkeys". Parkinsonism & related disorders 15 (6): 445–452. doi:10.1016/j.parkreldis.2008.11.001. PMID 19196540. edit

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[0] Rabiner, E. A.; Gunn, R. N.; Wilkins, M. R.; Sedman, E.; Grasby, P. M. (2002). "Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with 11CWAY-100635 and 11Craclopride". Journal of psychopharmacology (Oxford, England) 16 (3): 195–199. doi:10.1177/026988110201600301. PMID 12236624. edit

[1] Assié, M.; Ravailhe, V.; Faucillon, V.; Newman-Tancredi, A. (2005). "Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain". The Journal of pharmacology and experimental therapeutics 315 (1): 265–272. doi:10.1124/jpet.105.087163. PMID 15987834. edit

[2] Auclair, A.; Galinier, A.; Besnard, J.; Newman-Tancredi, A.; Depoortère, R. (2007). "Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats". Psychopharmacology 193 (1): 45–54. doi:10.1007/s00213-007-0762-7. PMID 17393144. edit

[3] Bibbiani, F.; Oh, J. D.; Chase, T. N. (2001). "Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models". Neurology 57 (10): 1829–1834. PMID 11723272. edit

[4] Bartoszyk, G.; Van Amsterdam, C.; Greiner, H.; Rautenberg, W.; Russ, H.; Seyfried, C. (2004). "Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile". Journal of neural transmission (Vienna, Austria : 1996) 111 (2): 113–126. doi:10.1007/s00702-003-0094-7. PMID 14767715. edit

[5] Bara-Jimenez, W.; Bibbiani, F.; Morris, M.; Dimitrova, T.; Sherzai, A.; Mouradian, M.; Chase, T. (2005). "Effects of serotonin 5-HT1A agonist in advanced Parkinson's disease". Movement disorders : official journal of the Movement Disorder Society 20 (8): 932–936. doi:10.1002/mds.20370. PMID 15791634. edit

[6] Grégoire, L.; Samadi, P.; Graham, J.; Bédard, P.; Bartoszyk, G.; Di Paolo, T. (2009). "Low doses of sarizotan reduce dyskinesias and maintain antiparkinsonian efficacy of L-Dopa in parkinsonian monkeys". Parkinsonism & related disorders 15 (6): 445–452. doi:10.1016/j.parkreldis.2008.11.001. PMID 19196540. edit

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Sarizotan

[edit] See also

[edit] References

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