Osanetant (SR-142,801) je antagonist neurokininskog 3 receptora koji je razvio Sanofi-Synthélabo, koji je istražuje kao mogući tretman za šizovreniju.[3] To je bio prvi ne-peptidni NK3 antagonist koji je razvijen tokom sredine 1990-tih,[4] ali još uvek nije dosegao tržište, mada su klinička ispitivanja nastavljaju.[5] Još jedna moguća primena osanetanta je u treatmanu bolesti zavisnosti, pošto je utvrđeno da blokira efekte kokaina u životinjskim modelima.[6][7]
Osanetant
|
| (IUPAC) ime
|
| N-(13-[(3R)-1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]propyl4-phenylpiperidin-4-yl]-N-methylacetamide
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| Klinički podaci
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| Identifikatori
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| CAS broj
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160492-56-8
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| ATC kod
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nije dodeljen
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| PubChem[1][2]
|
219077
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| Hemijski podaci
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| Formula
|
C35H41Cl2N3O2
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| Mol. masa
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606.625 g/mol
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| SMILES
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eMolekuli & PubHem
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| InChI |
|---|
InChI=1S/C35H41Cl2N3O2/c1-27(41)38(2)35(29-13-7-4-8-14-29)19-23-39(24-20-35)21-9-17-34(30-15-16-31(36)32(37)25-30)18-10-22-40(26-34)33(42)28-11-5-3-6-12-28/h3-8,11-16,25H,9-10,17-24,26H2,1-2H3/t34-/m0/s1  Y
Key: DZOJBGLFWINFBF-UMSFTDKQSA-N Y |
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| Farmakoinformacioni podaci
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| Trudnoća
|
?
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| Pravni status
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|
Literatura
uredi
- ↑ 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.
- ↑ Kamali F. Osanetant Sanofi-Synthélabo. Current Opinion in Investigational Drugs. 2001 Jul;2(7):950-6. PMID 11757797
- ↑ Emonds-Alt X, Bichon D, Ducoux JP, Heaulme M, Miloux B, Poncelet M, Proietto V, Van Broeck D, Vilain P, Neliat G, et al. SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor. Life Sciences. 1995;56(1):PL27-32. PMID 7830490
- ↑ Quartara L, Altamura M (August 2006). „Tachykinin receptors antagonists: from research to clinic”. Current Drug Targets 7 (8): 975–92. PMID 16918326. Arhivirano iz originala na datum 2011-07-25. Pristupljeno 2011-04-14.
- ↑ De Souza Silva MA, Mello EL Jr, Müller CP, Jocham G, Maior RS, Huston JP, Tomaz C, Barros M. The tachykinin NK3 receptor antagonist SR142801 blocks the behavioral effects of cocaine in marmoset monkeys. European Journal of Pharmacology. 2006 May 1;536(3):269-78. PMID 16603151
- ↑ Jocham G, Lezoch K, Müller CP, Kart-Teke E, Huston JP, de Souza Silva MA. Neurokinin receptor antagonism attenuates cocaine's behavioural activating effects yet potentiates its dopamine-enhancing action in the nucleus accumbens core. European Journal of Neuroscience. 2006 Sep;24(6):1721-32. PMID 17004936
Spoljašnje veze
uredi
