SB-277011-A — разлика између измена
Садржај обрисан Садржај додат
м DEFAULTSORT → СОРТИРАЊЕ |
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-{'''SB-277,011A'''}- je lek koji deluje kao potentan i selektivan [[antagonist (farmakologija)|antagonist]] [[dopamin]]kog [[Dopaminski receptor D3|D<sub>3</sub> receptor]] [[Receptor (biohemija)|receptora]].<ref>{{cite journal | |
-{'''SB-277,011A'''}- je lek koji deluje kao potentan i selektivan [[antagonist (farmakologija)|antagonist]] [[dopamin]]kog [[Dopaminski receptor D3|D<sub>3</sub> receptor]] [[Receptor (biohemija)|receptora]].<ref>{{cite journal |vauthors=Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, Nash DJ, Thewlis KM, Vong AK | title = Design and synthesis of trans-N-4-2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethylcyclohexyl-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat | journal = Journal of medicinal chemistry | volume = 43 | issue = 9 | pages = 1878–85 | year = 2000 | pmid = 10794704 | doi=10.1021/jm000090i}}</ref> On je oko 80-100 puta selektivniji za D<sub>3</sub> u odnosu na D<sub>2</sub>.<ref>{{cite journal |vauthors=Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN | title = Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain | journal = Brain research | volume = 1149 | pages = 50–7 | year = 2007 | pmid = 17382304 | doi = 10.1016/j.brainres.2007.02.051 }}</ref> On nije [[parcijalni agonist]].<ref>{{cite journal |vauthors=Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J | title = Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A | journal = The Journal of pharmacology and experimental therapeutics | volume = 294 | issue = 3 | pages = 1154–65 | year = 2000 | pmid = 10945872 }}</ref> |
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-{SB-277,011A}- se koristi za studiranje [[zavisnost|adikcije]] na [[psihostimulansi|stimulišuće]] droge poput [[nikotin]]a<ref>{{cite journal | |
-{SB-277,011A}- se koristi za studiranje [[zavisnost|adikcije]] na [[psihostimulansi|stimulišuće]] droge poput [[nikotin]]a<ref>{{cite journal |vauthors= ((Le Foll B)), Schwartz JC, Sokoloff P | title = Disruption of nicotine conditioning by dopamine D(3) receptor ligands | journal = Molecular psychiatry | volume = 8 | issue = 2 | pages = 225–30 | year = 2003 | pmid = 12610655 | doi = 10.1038/sj.mp.4001202 }}</ref> i [[kokain]]a.<ref>{{cite journal |vauthors=Vorel SR, ((Ashby Jr CR)), Paul M, Liu X, Hayes R, Hagan JJ, Middlemiss DN, Stemp G, Gardner EL | title = Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats | journal = Journal of Neuroscience | volume = 22 | issue = 21 | pages = 9595–603 | year = 2002 | pmid = 12417684 }}</ref><ref>{{cite journal |vauthors=Di Ciano P, Underwood RJ, Hagan JJ, Everitt BJ | title = Attenuation of cue-controlled cocaine-seeking by a selective D3 dopamine receptor antagonist SB-277011-A | journal = Neuropsychopharmacology | volume = 28 | issue = 2 | pages = 329–38 | year = 2003 | pmid = 12589386 | doi = 10.1038/sj.npp.1300148 }}</ref> |
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== Reference == |
== Reference == |
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== Spoljašnje veze == |
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{{Portal-lat|Medicina|Hemija}} |
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{{normativna kontrola}} |
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{{СОРТИРАЊЕ:SB-277011-A}} |
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[[Категорија:Допамински агонисти]] |
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[[Категорија:Хинолини]] |
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[[Категорија:Амиди]] |
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[[Категорија:Нитрили]] |
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[[Категорија:Тетрахидроизохинолини]] |
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Тренутна верзија на датум 15. октобар 2024. у 23:13
{{Drugbox-lat | Verifiedfields = | verifiedrevid = 449588534 | IUPAC_name = -{Ntrans-4-[2-(6-cijano-3,4-dihidroizohinolin-2(1H)-il)etil]cikloheksil}hinolin-4-karboksamid | image = SB277011A.png | width = 260 | image2 = | width2 =
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| metabolism = | elimination_half-life = | excretion =
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| CAS_number =
| ATC_prefix =
| ATC_suffix =
| PubChem = 5311096
| IUPHAR_ligand = 143
| DrugBank_Ref =
| DrugBank =
| ChEMBL_Ref =
| ChEMBL = 85606
| C=28 | H=30 | N=4 | O=1
| molecular_weight =
| smiles = c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N
| StdInChI_Ref =
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| StdInChIKey_Ref =
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SB-277,011A je lek koji deluje kao potentan i selektivan antagonist dopaminkog D3 receptor receptora.[1] On je oko 80-100 puta selektivniji za D3 u odnosu na D2.[2] On nije parcijalni agonist.[3]
SB-277,011A se koristi za studiranje adikcije na stimulišuće droge poput nikotina[4] i kokaina.[5][6]
Reference
[уреди | уреди извор]- ^ Stemp G, Ashmeade T, Branch CL, Hadley MS, Hunter AJ, Johnson CN, Nash DJ, Thewlis KM, Vong AK (2000). „Design and synthesis of trans-N-4-2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethylcyclohexyl-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat”. Journal of medicinal chemistry. 43 (9): 1878—85. PMID 10794704. doi:10.1021/jm000090i.
- ^ Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN (2007). „Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain”. Brain research. 1149: 50—7. PMID 17382304. doi:10.1016/j.brainres.2007.02.051.
- ^ Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J (2000). „Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A”. The Journal of pharmacology and experimental therapeutics. 294 (3): 1154—65. PMID 10945872.
- ^ Le Foll B, Schwartz JC, Sokoloff P (2003). „Disruption of nicotine conditioning by dopamine D(3) receptor ligands”. Molecular psychiatry. 8 (2): 225—30. PMID 12610655. doi:10.1038/sj.mp.4001202.
- ^ Vorel SR, Ashby Jr CR, Paul M, Liu X, Hayes R, Hagan JJ, Middlemiss DN, Stemp G, Gardner EL (2002). „Dopamine D3 receptor antagonism inhibits cocaine-seeking and cocaine-enhanced brain reward in rats”. Journal of Neuroscience. 22 (21): 9595—603. PMID 12417684.
- ^ Di Ciano P, Underwood RJ, Hagan JJ, Everitt BJ (2003). „Attenuation of cue-controlled cocaine-seeking by a selective D3 dopamine receptor antagonist SB-277011-A”. Neuropsychopharmacology. 28 (2): 329—38. PMID 12589386. doi:10.1038/sj.npp.1300148.
