SB 277011A dihydrochloride (Synonyms: SB-277011A dihydrochloride) |
| Catalog No.GC13183 |
Le dichlorhydrate de SB 277011A (dichlorhydrate de SB-277011A) est un antagoniste puissant, sélectif, biodisponible par voie orale et pénétrant dans le cerveau des récepteurs de la dopamine D3, avec des pKis de 8,0, 6,0, <5,2 et 5,9 pour les récepteurs D3, D2, 5-HT1B et 5-HT1D , respectivement.
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Cas No.: 1226917-67-4
Sample solution is provided at 25 µL, 10mM.
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SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1].
SB-277011 dihydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].
References:
[1]. Stemp G, et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4;43(9):1878-85.
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