Kotinin

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Kotinin
(IUPAC) ime
(5S)-1-metil-5-(3-piridil)pirolidin-2-on
Klinički podaci
Identifikatori
CAS broj 486-56-6
ATC kod nije dodeljen
PubChem[1][2] 854019
ChemSpider[3] 746405
UNII K5161X06LL DaY
ChEMBL[4] CHEMBL578211 DaY
Hemijski podaci
Formula C10H12N2O 
Mol. masa 176,22 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Poluvreme eliminacije 20 sata
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene Oralno, pušenjem

Kotinin je alkaloid prisutan u duvanu i kao metabolit nikotina.[5][6] Reč "kotinin" je anagram "nikotina". Kotinin se koristi kao biomarker za izlaganje duvanskom dimu. On je u prodaji kao antidepresiv pod imenom Scotine.[5]

Slično nikotinu, kotinin se vezuje za, aktivira, i desenzituje neuronski nikotinske acetilholinske receptore, mada sa znatno nižom potentnošću.[6][7][8][9] On ispoljava nootropne i antipsihoticima slične efekte.[10][11]

Reference[uredi | uredi kod]

  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. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. 5,0 5,1 Triggle, David J. (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. ISBN 0-412-46630-9. 
  6. 6,0 6,1 Dwoskin LP, Teng L, Buxton ST, Crooks PA (March 1999). „(S)-(-)-Cotinine, the major brain metabolite of nicotine, stimulates nicotinic receptors to evoke [3Hdopamine release from rat striatal slices in a calcium-dependent manner”]. The Journal of Pharmacology and Experimental Therapeutics 288 (3): 905–11. PMID 10027825. 
  7. Anderson DJ, Arneric SP (March 1994). „Nicotinic receptor binding of [3Hcytisine, [3H]nicotine and [3H]methylcarbamylcholine in rat brain”]. European Journal of Pharmacology 253 (3): 261–7. DOI:10.1016/0014-2999(94)90200-3. PMID 8200419. 
  8. Briggs CA, McKenna DG (September 1998). „Activation and inhibition of the human alpha7 nicotinic acetylcholine receptor by agonists”. Neuropharmacology 37 (9): 1095–102. DOI:10.1016/S0028-3908(98)00110-5. PMID 9833639. 
  9. Buccafusco JJ, Shuster LC, Terry AV (February 2007). „Disconnection between activation and desensitization of autonomic nicotinic receptors by nicotine and cotinine”. Neuroscience Letters 413 (1): 68–71. DOI:10.1016/j.neulet.2006.11.028. PMID 17157984. 
  10. Buccafusco JJ, Terry AV (October 2009). „A reversible model of the cognitive impairment associated with schizophrenia in monkeys: potential therapeutic effects of two nicotinic acetylcholine receptor agonists”. Biochemical Pharmacology 78 (7): 852–62. DOI:10.1016/j.bcp.2009.06.102. PMID 19577545. 
  11. Buccafusco JJ, Beach JW, Terry AV (February 2009). „Desensitization of nicotinic acetylcholine receptors as a strategy for drug development”. The Journal of Pharmacology and Experimental Therapeutics 328 (2): 364–70. DOI:10.1124/jpet.108.145292. PMC 2682277. PMID 19023041. 

Literatura[uredi | uredi kod]

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