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Systematic (IUPAC) name
Clinical data
Legal status
  • Uncontrolled
CAS number 137275-80-0
ATC code ?
PubChem CID 198746
ChemSpider 172023 YesY
UNII M65825806Q YesY
Chemical data
Formula C20H23NO4 
Mol. mass 341.400 g/mol
 YesY (what is this?)  (verify)

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[edit]


  1. ^ Matsuda, T.; Yoshikawa, T.; Suzuki, M.; Asano, S.; Somboonthum, P.; Takuma, K.; Nakano, Y.; Morita, T.; Nakasu, Y.; Kim, H. S.; Egawa, M.; Tobe, A.; Baba, A. (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): 357–366. 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): 141–144. doi:10.1016/S0014-2999(02)02786-3. PMID 12498918.  edit
  4. ^ Sakaue, M.; Somboonthum, P.; Nishihara, B.; Koyama, Y.; Hashimoto, H.; Baba, A.; Matsuda, T. (2000). "Postsynaptic 5-hydroxytryptamine1A 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 1571922. 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): 1050–1056. 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. doi:10.1254/jphs.FM0070121. 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. doi:10.1254/jphs.08297FP. 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): 728–731. doi:10.1248/bpb.32.728. PMID 19336914.  edit