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Chemical Compound Review

AGN-PC-0D9KVV     1-chroman-2-yl-N-[[5-(4...

Synonyms: SureCN311845, AC1MHW5N, DCL000973, LS-192590, CID3058747, ...
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Disease relevance of Sarizotan


Psychiatry related information on Sarizotan


High impact information on Sarizotan

  • METHODS: The 5-HT1A receptor agonist sarizotan (EMD128130) was systemically administered alone and together with levodopa to parkinsonian rats and nonhuman primates [1].
  • When 5-HT1A receptors were blocked by pretreatment with WAY100635 (2.5 mg/kg, s.c.), cataleptogenic properties of SSR181507 and sarizotan were unmasked, and the catalepsy induced by bifeprunox was enhanced [2].
  • Results from clinical trials suggest that sarizotan significantly alleviates levodopa-induced dyskinesia [3].
  • Here we report the functional effects of sarizotan on human D2-like dopamine receptors (D2S, D2L, D3, D4.2 and D4.4) individually expressed in the AtT-20 neuroendocrine cell line [3].
  • RESULTS: After administration of sarizotan, a significant reduction of REM sleep and total sleep time in conventional sleep EEG and a significant reduction of sigma- and theta-power in spectral analysis were observed [4].

Chemical compound and disease context of Sarizotan


Biological context of Sarizotan

  • CONCLUSIONS: At a dose higher than that intended for clinical use (1 mg b.i.d.), sarizotan had no effect on the metabolism and pharmacokinetics of specific probe drugs for CYP isoenzymes 1A2, 2C19, 2C9, 2D6 and 3A4 [7].

Anatomical context of Sarizotan

  • In medial prefrontal cortex, dopamine levels were increased by SSR181507, SLV313, sarizotan, and (+)8-OH-DPAT [8].
  • These findings suggest that the anti-dyskinetic properties of sarizotan could be mediated via its 5-HT(1A) agonist actions in the motor cortex, leading to reduced activity in the corticostriatal glutamate pathways with reduced activation of the striatopallidal GABA pathway mediating motor inhibition [9].
  • However, sarizotan at higher doses decreased DA precursor accumulation in reserpinized rats and induced contralateral rotational behavior in unilaterally substantia nigra lesioned rats, indicating some intrinsic dopaminergic activity; at D2 receptors sarizotan may act as a partial agonist, depending on the dopaminergic impulse flow [10].

Associations of Sarizotan with other chemical compounds

  • The effects of sarizotan, a 5-HT(1A) agonist with additional affinity for D(3) and D(4) receptors, have been studied on the corticostriatal glutamate pathways using dual-probe microdialysis in the awake rat [9].

Gene context of Sarizotan

  • We investigated the effect of sarizotan on the clinical pharmacokinetics of probe drugs for cytochrome P450 (CYP) to evaluate the risk of CYP-related drug-drug interactions [7].
  • To evaluate this hypothesis, effects of a selective 5-HT1A agonist, sarizotan, given orally at 2 and 5 mg twice daily to 18 relatively advanced parkinsonian patients, were compared with baseline placebo function during a 3-week, double-blind, placebo-controlled, proof-of-concept study [11].


  1. Serotonin 5-HT1A agonist improves motor complications in rodent and primate parkinsonian models. Bibbiani, F., Oh, J.D., Chase, T.N. Neurology (2001) [Pubmed]
  2. Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties. Bardin, L., Kleven, M.S., Barret-Grévoz, C., Depoortère, R., Newman-Tancredi, A. Neuropsychopharmacology (2006) [Pubmed]
  3. The novel antidyskinetic drug sarizotan elicits different functional responses at human D2-like dopamine receptors. Kuzhikandathil, E.V., Bartoszyk, G.D. Neuropharmacology (2006) [Pubmed]
  4. Changes in sleep electroencephalogram and nocturnal hormone secretion after administration of the antidyskinetic agent sarizotan in healthy young male volunteers. Kuenzel, H.E., Steiger, A., Held, K., Antonijevic, I.A., Frieboes, R.M., Murck, H. Psychopharmacology (Berl.) (2005) [Pubmed]
  5. Novel antipsychotic agents with 5-HT(1A) agonist properties: role of 5-HT(1A) receptor activation in attenuation of catalepsy induction in rats. Kleven, M.S., Barret-Grévoz, C., Slot, L.B., Newman-Tancredi, A. Neuropharmacology (2005) [Pubmed]
  6. In 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Primates, the Selective 5-Hydroxytryptamine 1a Agonist (R)-(+)-8-OHDPAT Inhibits Levodopa-Induced Dyskinesia but Only with\ Increased Motor Disability. Iravani, M.M., Tayarani-Binazir, K., Chu, W.B., Jackson, M.J., Jenner, P. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  7. Investigation of sarizotan's impact on the pharmacokinetics of probe drugs for major cytochrome P450 isoenzymes: a combined cocktail trial. Krösser, S., Neugebauer, R., Dolgos, H., Fluck, M., Rost, K.L., Kovar, A. Eur. J. Clin. Pharmacol. (2006) [Pubmed]
  8. Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical dopamine and hippocampal serotonin release in rat brain. Assié, M.B., Ravailhe, V., Faucillon, V., Newman-Tancredi, A. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  9. Effects of sarizotan on the corticostriatal glutamate pathways. Antonelli, T., Fuxe, K., Tomasini, M.C., Bartoszyk, G.D., Seyfried, C.A., Tanganelli, S., Ferraro, L. Synapse (2005) [Pubmed]
  10. Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile. Bartoszyk, G.D., Van Amsterdam, C., Greiner, H.E., Rautenberg, W., Russ, H., Seyfried, C.A. Journal of neural transmission (Vienna, Austria : 1996) (2004) [Pubmed]
  11. Effects of serotonin 5-HT1A agonist in advanced Parkinson's disease. Bara-Jimenez, W., Bibbiani, F., Morris, M.J., Dimitrova, T., Sherzai, A., Mouradian, M.M., Chase, T.N. Mov. Disord. (2005) [Pubmed]
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