SB-277011-A

{{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

| tradename = | legal_status = | routes_of_administration =

| metabolism = | elimination_half-life = | excretion =

| C=28 | H=30 | N=4 | O=1 | molecular_weight = 438,563 g/mol | smiles = c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N }}

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

^ 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.

[1] 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.

[2] 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.

[3] 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.

[4] 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.

[5] 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.

[6] 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.

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