CP-94,253 je lek koji deluje kao potentan i selektivan agonist serotoninskog 5-HT1B receptora, sa aproksimativno 25x i 40x selektivnošću u odnosu na blisko srodne 5-HT1D i 5-HT1A receptore.[3] On pokazuje opseg biheviouralnih efekata u životinjskim studijama, uključujući promovisanje budnosti putem povećanja dopaminskog otpuštanja u mozgu,[4][5] redukovanje unosa hrane i povećanja sitosti,[6][7][8] pojačanja dejstva kokaina,[9][10][11][12] kao i moguće antidepresivno dejstvo.[13]
CP-94,253
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(IUPAC) ime
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3-(1,2,5,6-tetrahidro-4-piridil)-5-propoksipirolo[3,2-b]piridin
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Klinički podaci
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Identifikatori
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CAS broj
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131084-35-0
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ATC kod
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nije dodeljen
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PubChem[1][2]
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4029677
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Hemijski podaci
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Formula
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C15H19N3O
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Mol. masa
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257,330 g/mol
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SMILES
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eMolekuli & PubHem
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InChI |
InChI=1S/C15H19N3O/c1-2-9-19-14-4-3-13-15(18-14)12(10-17-13)11-5-7-16-8-6-11/h3-5,10,16-17H,2,6-9H2,1H3 Key: KWQWBZIGHIOKIO-UHFFFAOYSA-N Y |
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Farmakoinformacioni podaci
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Trudnoća
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?
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Pravni status
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- ↑ 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
- ↑ 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.
- ↑ Koe KB, Nielsen JA, Macor JE, Heym J. Biochemical and behavioral studies of the 5-HT1B receptor agonist, CP-94,253. Drug Development Research. 1992;26(3):241-250. DOI:10.1002/ddr.430260305
- ↑ Monti JM, Monti D, Jantos H, Ponzoni A. Effects of selective activation of the 5-HT1B receptor with CP-94,253 on sleep and wakefulness in the rat. Neuropharmacology. 1995 Dec;34(12):1647-51. PMID 8788962
- ↑ Iyer RN, Bradberry CW. Serotonin-mediated increase in prefrontal cortex dopamine release: pharmacological characterization. Journal of Pharmacology and Experimental Therapeutics. 1996 Apr;277(1):40-7. PMID 8613947
- ↑ Halford JC, Blundell JE. The 5-HT1B receptor agonist CP-94,253 reduces food intake and preserves the behavioural satiety sequence. Physiology and Behaviour. 1996 Sep;60(3):933-9. PMID 8873272
- ↑ Lee MD, Simansky KJ. CP-94,253: a selective serotonin1B (5-HT1B) agonist that promotes satiety. Psychopharmacology (Berlin). 1997 Jun;131(3):264-70. PMID 9203237
- ↑ Lee MD, Kennett GA, Dourish CT, Clifton PG. 5-HT1B receptors modulate components of satiety in the rat: behavioural and pharmacological analyses of the selective serotonin1B agonist CP-94,253. Psychopharmacology (Berlin). 2002 Oct;164(1):49-60. PMID 12373419
- ↑ Parsons LH, Weiss F, Koob GF. Serotonin1B receptor stimulation enhances cocaine reinforcement. Journal of Neuroscience. 1998 Dec 1;18(23):10078-89. PMID 9822762
- ↑ Przegalinski E, Filip M, Papla I, Siwanowicz J. Effect of serotonin (5-HT)1B receptor ligands on cocaine sensitization in rats. Behavioural Pharmacology. 2001 Apr;12(2):109-16. PMID 11396515
- ↑ Przegaliński E, Gołda A, Frankowska M, Zaniewska M, Filip M (March 2007). „Effects of serotonin 5-HT1B receptor ligands on the cocaine- and food-maintained self-administration in rats”. European Journal of Pharmacology 559 (2-3): 165–72. DOI:10.1016/j.ejphar.2006.12.012. PMID 17291490.
- ↑ Przegaliński E, Gołda A, Filip M (2008). „Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats”. Pharmacological Reports : PR 60 (6): 798–810. PMID 19211971.
- ↑ Tatarczyńska E, Antkiewicz-Michaluk L, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E. Antidepressant-like effect of the selective 5-HT1B receptor agonist CP 94253: a possible mechanism of action. European Journal of Pharmacology. 2005 May 23;516(1):46-50. PMID 15913599