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SB-277011-A

Izvor: Wikipedija
(Preusmjereno sa stranice SB-277,011-A)
SB-277011-A
(IUPAC) ime
N'trans-4-[2-(6-cijano-3,4-dihidroizohinolin-2(1H)-il)etil]cikloheksil
Klinički podaci
Identifikatori
ATC kod ?
Hemijski podaci
Formula ?
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

hinolin-4-karboksamid

| image = SB277011A.png | width = 260 | image2 = | width2 =

| tradename = | legal_status = | routes_of_administration =

| metabolism = | elimination_half-life = | excretion =

| CAS_number_Ref =  DaY | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = 5311096 | IUPHAR_ligand = 143 | DrugBank_Ref = Šablon:Drugbankcite | DrugBank = | ChEMBL_Ref =  DaY | ChEMBL = 85606

| C=28 | H=30 | N=4 | O=1 | molecular_weight = 438,563 g/mol | smiles = c4cccc1c4nccc1C(=O)NC3CCC(CC3)CCN(CCc2c5)Cc2ccc5C#N | InChI = | InChIKey = | StdInChI_Ref =  DaY | StdInChI = 1S/C28H30N4O/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33) | StdInChIKey_Ref =  DaY | StdInChIKey = OLWRVVHPJFLNPW-UHFFFAOYSA-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

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  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. DOI:10.1021/jm000090i. PMID 10794704. 
  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. DOI:10.1016/j.brainres.2007.02.051. PMID 17382304. 
  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. DOI:10.1038/sj.mp.4001202. PMID 12610655. 
  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. DOI:10.1038/sj.npp.1300148. PMID 12589386. 

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