SB-242,084
 | |
| IUPAC ime | |
|---|---|
6-hloro-5-metil-N-{6-[(2-metilpiridin-3-il)oksi]piridin-3-il]indolin-1-karboksamid | |
| Identifikatori | |
| CAS broj | 181632-25-7 |
| ATC kod | none |
| PubChem | CID 3644637 |
| IUPHAR/BPS | 193 |
| ChEMBL | CHEMBL14563 |
| Hemijski podaci | |
| Formula | C21H19ClN4O2 |
| Molarna masa | 394,853 g/mol |
| |
SB-242,084 je psihoaktivni lek i istraživačka hemikalija koja deluje kao selektivni antagonist za 5HT2C receptor.[1] On ima anksiolitičko dejstvo,[2] i pojačava dopaminsku signalizaciju u limbičnom sistemu.[3] On takođe ima kompleksno dejstvo na otpuštanje dopamina proizvedeno kokainom, povećavajući ga u pojedinim delovima mozga[4][5] i snižavajući ga u drugim.[6][7] Pokazano je da povišava efektivnost selektivnih inhibitora preuzimanja serotonina (SSRI), i da redukuje njihove nuspojave.[8][9] U životinjskim studijama, SB-242,084 proizvodi stimulansnu aktivnost, koja je donekle slična ali znatno slabija od kokaina i amfetamina.[10]
Vidi još[uredi | uredi izvor]
Reference[uredi | uredi izvor]
- ^ Kennett, GA; Wood, MD; Bright, F; Trail, B; Riley, G; Holland, V; Avenell, KY; Stean, T; Upton, N (1997). „SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist”. Neuropharmacology. 36 (4–5): 609—20. PMID 9225286. doi:10.1016/S0028-3908(97)00038-5.
- ^ Martin, JR; Ballard, TM; Higgins, GA (2002). „Influence of the 5-HT2C receptor antagonist, SB-242084, in tests of anxiety”. Pharmacology, Biochemistry, and Behavior. 71 (4): 615—25. PMID 11888553. doi:10.1016/S0091-3057(01)00713-4.
- ^ Di Matteo, V; Di Giovanni, G; Di Mascio, M; Esposito, E (1999). „SB 242084, a selective serotonin2C receptor antagonist, increases dopaminergic transmission in the mesolimbic system”. Neuropharmacology. 38 (8): 1195—205. PMID 10462132. doi:10.1016/S0028-3908(99)00047-7.
- ^ Navailles, S; De Deurwaerdère, P; Porras, G; Spampinato, U (2004). „In vivo evidence that 5-HT2C receptor antagonist but not agonist modulates cocaine-induced dopamine outflow in the rat nucleus accumbens and striatum”. Neuropsychopharmacology. 29 (2): 319—26. PMID 14560323. doi:10.1038/sj.npp.1300329.
- ^ Navailles, S; Moison, D; Ryczko, D; Spampinato, U (2006). „Region-dependent regulation of mesoaccumbens dopamine neurons in vivo by the constitutive activity of central serotonin2C receptors”. Journal of Neurochemistry. 99 (4): 1311—9. PMID 17018023. doi:10.1111/j.1471-4159.2006.04188.x.
- ^ Navailles, S; Moison, D; Cunningham, KA; Spampinato, U (2008). „Differential regulation of the mesoaccumbens dopamine circuit by serotonin2C receptors in the ventral tegmental area and the nucleus accumbens: an in vivo microdialysis study with cocaine”. Neuropsychopharmacology. 33 (2): 237—46. PMID 17429406. doi:10.1038/sj.npp.1301414.
- ^ Leggio, GM; Cathala, A; Moison, D; Cunningham, KA; Piazza, PV; Spampinato, U (2009). „Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens”. Neuropharmacology. 56 (2): 507—13. PMC 3130963
. PMID 18977370. doi:10.1016/j.neuropharm.2008.10.005.
- ^ Cremers, TI; Giorgetti, M; Bosker, FJ; Hogg, S; Arnt, J; Mørk, A; Honig, G; Bøgesø, KP; Westerink, BH (2004). „Inactivation of 5-HT(2C) receptors potentiates consequences of serotonin reuptake blockade”. Neuropsychopharmacology. 29 (10): 1782—9. PMID 15138437. doi:10.1038/sj.npp.1300474.
- ^ Burghardt, NS; Bush, DE; McEwen, BS; Ledoux, JE (2007). „Acute SSRIs Increase Conditioned Fear Expression: Blockade with a 5-HT2C Receptor Antagonist”. Biological Psychiatry. 62 (10): 1111—8. PMC 2129095 . PMID 17524369. doi:10.1016/j.biopsych.2006.11.023.
- ^ Manvich, D. F.; Kimmel, H. L.; Cooper, D. A.; Howell, L. L. (2012). „The Serotonin 2C Receptor Antagonist SB 242084 Exhibits Abuse-Related Effects Typical of Stimulants in Squirrel Monkeys”. Journal of Pharmacology and Experimental Therapeutics. PMID 22685342. doi:10.1124/jpet.112.195156.
