Osemozotan

Osemozotan (MKC-242) je selektivni agonist 5-HT_1A receptora sa funkcionalnom selektivnošću. On deluje kao pun agonist na presinaptičkim i kao parcijalni agonist na postsinaptičkim 5-HT_1A receptorima.^[3] On pokazuje antidepresivne i anksiolitske efekte u životinjskim studijama.^[4][5] Osemozotan se koristi za istraživanje uloge 5-HT_1A receptora u modulaciji otpuštanja dopamina i serotonina u mozgu,^[6][7] i njihovog učešća u adikciji na zloupotrebljene stimulante kao što su kokain i metamfetamin.^{[8][9][10][11][12]}

Osemozotan

(IUPAC) ime
5-(3-[((2S)-1,4-benzodioksan-2-ilmetil)amino]propoksi)-1,3-benzodioksol
Klinički podaci
Identifikatori
CAS broj	137275-80-0
ATC kod	nije dodeljen
PubChem[1][2]	198746
UNII	M65825806Q Y
Hemijski podaci
Formula	C20H23NO4
Mol. masa	341,400 g/mol
SMILES	eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Nije kontrolisana supstanca

Reference

1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
3. Matsuda, T.; Yoshikawa, T.; Suzuki, M.; Asano, S.; Somboonthum, P.; Takuma, K.; Nakano, Y.; Morita, T. i dr.. (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.
4. 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.
5. 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.
6. 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.
7. 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.
8. 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.
9. 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.
10. 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.
11. Tsuchida, R.; Kubo, M.; Kuroda, M.; Shibasaki, Y.; Shintani, N.; Abe, M.; Köves, K.; Hashimoto, H. i dr.. (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.
12. Tsuchida, R.; Kubo, M.; Shintani, N.; Abe, M.; Köves, K.; Uetsuki, K.; Kuroda, M.; Hashimoto, H. i dr.. (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.

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