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Systematic (IUPAC) name
Legal status
Legal status
  • Uncontrolled
CAS Number 137275-80-0
PubChem CID 198746
Chemical data
Formula C20H23NO4
Molar mass 341.400 g/mol[[Script error: No such module "String".]]
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Osemozotan (MKC-242) is a selective 5-HT1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT1A receptors.[1] It has antidepressant and anxiolytic effects in animal studies,[2][3] and is used to investigate the role of 5-HT1A receptors in modulating the release of dopamine and serotonin in the brain,[4][5] and their involvement in addiction to abused stimulants such as cocaine and methamphetamine.[6][7][8][9][10]

See also


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  1. Matsuda, T; Yoshikawa, T; Suzuki, M; Asano, S; Somboonthum, P; Takuma, K; Nakano, Y; Morita, T; Nakasu, Y (1995). "Novel benzodioxan derivative, 5-(3-((2S)-1,4-benzodioxan-2- ylmethyl)aminopropoxy)-1,3-benzodioxole HCl (MKC-242), with a highly potent and selective agonist activity at rat central serotonin1A receptors". Japanese journal of pharmacology. 69 (4): 357–66. doi:10.1254/jjp.69.357. PMID 8786639.  edit
  2. Abe, M; Tabata, R; Saito, K; Matsuda, T; Baba, A; Egawa, M (1996). "Novel benzodioxan derivative, 5-3-((2S)-1,4-benzodioxan-2-ylmethyl) aminopropoxy-1,3-benzodioxole HCl (MKC-242), with anxiolytic-like and antidepressant-like effects in animal models". The Journal of pharmacology and experimental therapeutics. 278 (2): 898–905. PMID 8768745.  edit
  3. Sakaue, M; Ago, Y; Sowa, C; Koyama, Y; Baba, A; Matsuda, T (2003). "The 5-HT1A receptor agonist MKC-242 increases the exploratory activity of mice in the elevated plus-maze". European journal of pharmacology. 458 (1-2): 141–4. PMID 12498918.  edit
  4. Sakaue, M.; Somboonthum, P.; Nishihara, B.; Koyama, Y.; Hashimoto, H.; Baba, A.; Matsuda, T. (2000). "Postsynaptic 5-hydroxytryptamine(1A) receptor activation increases in vivo dopamine release in rat prefrontal cortex". British journal of pharmacology. 129 (5): 1028–1034. doi:10.1038/sj.bjp.0703139. PMC 1571922Freely accessible. PMID 10696105.  edit
  5. Ago, Y; Koyama, Y; Baba, A; Matsuda, T (2003). "Regulation by 5-HT1A receptors of the in vivo release of 5-HT and DA in mouse frontal cortex". Neuropharmacology. 45 (8): 1050–6. doi:10.1016/S0028-3908(03)00304-6. PMID 14614948.  edit
  6. Ago, Y.; Nakamura, S.; Uda, M.; Kajii, Y.; Abe, M.; Baba, A.; Matsuda, T. (2006). "Attenuation by the 5-HT1A receptor agonist osemozotan of the behavioral effects of single and repeated methamphetamine in mice". Neuropharmacology. 51 (4): 914–922. doi:10.1016/j.neuropharm.2006.06.001. PMID 16863654.  edit
  7. Ago, Y.; Nakamura, S.; Hayashi, A.; Itoh, S.; Baba, A.; Matsuda, T. (2006). "Effects of osemozotan, ritanserin and azasetron on cocaine-induced behavioral sensitization in mice". Pharmacology, biochemistry, and behavior. 85 (1): 198–205. doi:10.1016/j.pbb.2006.07.036. PMID 16962650.  edit
  8. Ago, Y; Nakamura, S; Baba, A; Matsuda, T (2008). "Neuropsychotoxicity of abused drugs: effects of serotonin receptor ligands on methamphetamine- and cocaine-induced behavioral sensitization in mice". Journal of pharmacological sciences. 106 (1): 15–21. PMID 18198473.  edit
  9. Tsuchida, R; Kubo, M; Kuroda, M; Shibasaki, Y; Shintani, N; Abe, M; Köves, K; Hashimoto, H; Baba, A (2009). "An antihyperkinetic action by the serotonin 1A-receptor agonist osemozotan co-administered with psychostimulants or the non-stimulant atomoxetine in mice". Journal of pharmacological sciences. 109 (3): 396–402. PMID 19270432.  edit
  10. Tsuchida, R; Kubo, M; Shintani, N; Abe, M; Köves, K; Uetsuki, K; Kuroda, M; Hashimoto, H; Baba, A (2009). "Inhibitory effects of osemozotan, a serotonin 1A-receptor agonist, on methamphetamine-induced c-Fos expression in prefrontal cortical neurons". Biological & pharmaceutical bulletin. 32 (4): 728–31. doi:10.1248/bpb.32.728. PMID 19336914.  edit