Kotinin
Kotinin je alkaloid prisutan u duvanu i kao metabolit nikotina.[1][2] Reč "kotinin" je anagram "nikotina". Kotinin se koristi kao biomarker za izlaganje duvanskom dimu. On je u prodaji kao antidepresiv pod imenom Scotine.[1]
IUPAC ime | |
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(5S)-1-metil-5-(3-piridil)pirolidin-2-on | |
Klinički podaci | |
Način primene | Oralno, pušenjem |
Pravni status | |
Pravni status |
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Farmakokinetički podaci | |
Poluvreme eliminacije | 20 sata |
Identifikatori | |
CAS broj | 486-56-6 |
ATC kod | none |
PubChem | CID 854019 |
ChemSpider | 746405 |
UNII | K5161X06LL |
ChEMBL | CHEMBL578211 |
Hemijski podaci | |
Formula | C10H12N2O |
Molarna masa | 176,22 g/mol |
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Slično nikotinu, kotinin se vezuje za, aktivira, i desenzituje neuronski nikotinske acetilholinske receptore, mada sa znatno nižom potentnošću.[2][3][4][5] On ispoljava nootropne i antipsihoticima slične efekte.[6][7]
Reference уреди
- ^ а б Triggle, David J. (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. ISBN 0-412-46630-9.
- ^ а б Dwoskin LP, Teng L, Buxton ST, Crooks PA (1999). „(S)-(-)-Cotinine, the major brain metabolite of nicotine, stimulates nicotinic receptors to evoke [3H]dopamine release from rat striatal slices in a calcium-dependent manner”. The Journal of Pharmacology and Experimental Therapeutics. 288 (3): 905—11. PMID 10027825.
- ^ Anderson DJ, Arneric SP (1994). „Nicotinic receptor binding of [3H]cytisine, [3H]nicotine and [3H]methylcarbamylcholine in rat brain”. European Journal of Pharmacology. 253 (3): 261—7. PMID 8200419. doi:10.1016/0014-2999(94)90200-3.
- ^ Briggs CA, McKenna DG (1998). „Activation and inhibition of the human alpha7 nicotinic acetylcholine receptor by agonists”. Neuropharmacology. 37 (9): 1095—102. PMID 9833639. doi:10.1016/S0028-3908(98)00110-5.
- ^ Buccafusco JJ, Shuster LC, Terry AV (2007). „Disconnection between activation and desensitization of autonomic nicotinic receptors by nicotine and cotinine”. Neuroscience Letters. 413 (1): 68—71. PMID 17157984. doi:10.1016/j.neulet.2006.11.028.
- ^ Buccafusco JJ, Terry AV (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. PMID 19577545. doi:10.1016/j.bcp.2009.06.102.
- ^ Buccafusco JJ, Beach JW, Terry AV (2009). „Desensitization of nicotinic acetylcholine receptors as a strategy for drug development”. The Journal of Pharmacology and Experimental Therapeutics. 328 (2): 364—70. PMC 2682277 . PMID 19023041. doi:10.1124/jpet.108.145292.