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Chemical Compound Review

CHEMBL85606     N-[4-[2-(6-cyano-3,4-dihydro- 1H...

Synonyms: cc-478, SureCN3099712, SureCN3099718, CS-0368, HY-10847, ...
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Disease relevance of SB 277011

  • In November 2000, data presented at the 30th Neuroscience meeting in New Orleans, LA, demonstrated that D3 receptor blockade with SB-277011 specifically altered neurochemical effects in the nucleus accumbens without the non-selective effects, such as catalepsy, seen with some other antagonists [390460] [1].

Psychiatry related information on SB 277011

  • In habituated rats, SB 277011 (13.5, 20 and 30 mg/kg p.o.) exerted no significant effects on motor activity and did not antagonize the hypoactivity caused by PD 128907 [2].

High impact information on SB 277011

  • Subsequent optimization of this new series to improve the cytochrome P450 inhibitory profile and CNS penetration gave trans-N-[4-[2-(6-cyano-1, 2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarbo xamide (24, SB-277011) [3].
  • The oral bioavailability of SB-277011 in rat, dog and cynomolgus monkey was 35, 43 and 2%, respectively [4].
  • 4. The in vivo pharmacokinetics showed that the plasma clearance of SB-277011 was low in rat (20 ml min(-1) kg(-1)), moderate in dog (14 ml min(-1) kg(-1)) and high in cynomolgus monkey (58 ml min(-1)kg(-1)), which is consistent with the in vitro findings and demonstrated a greater capacity for the monkey to metabolize this compound [4].
  • 2. In the presence of NADPH, SB-277011 was relatively stable in the presence of liver microsomes from rat, dog, cynomolgus monkey and human with an intrinsic clearance (CLi) of < 2 ml min(-1) g(-1) liver for all species [4].
  • 5. The high in vitro clearance of SB-277011 in human liver homogenates and the involvement of aldehyde oxidase in the metabolism of SB-277011 indicates that the bioavailability of the compound is likely to be low in human [4].

Chemical compound and disease context of SB 277011


Anatomical context of SB 277011

  • In total liver homogenates, SB-277011 was metabolized at a similar rate in rat and dog (CLi < 2 ml min(-1) g(-1) liver) to that in liver microsomes but in cynomolgus monkey and human (CLi = 9.9 and 45 ml min(-1) g(-1) liver, respectively) the intrinsic clearance was approximately 6- and 35-fold higher, respectively, than that in liver microsomes [4].

Associations of SB 277011 with other chemical compounds


  1. SB-277011 GlaxoSmithKline. Remington, G., Kapur, S. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
  2. Effects of dopamine D3 receptor antagonists on spontaneous and agonist-reduced motor activity in NMRI mice and Wistar rats: comparative study with nafadotride, U 99194A and SB 277011. Gyertyán, I., Sághy, K. Behavioural pharmacology. (2004) [Pubmed]
  3. 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. Stemp, G., Ashmeade, T., Branch, C.L., Hadley, M.S., Hunter, A.J., Johnson, C.N., Nash, D.J., Thewlis, K.M., Vong, A.K., Austin, N.E., Jeffrey, P., Avenell, K.Y., Boyfield, I., Hagan, J.J., Middlemiss, D.N., Reavill, C., Riley, G.J., Routledge, C., Wood, M. J. Med. Chem. (2000) [Pubmed]
  4. Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey: in vitro/in vivo correlation and the role of aldehyde oxidase. Austin, N.E., Baldwin, S.J., Cutler, L., Deeks, N., Kelly, P.J., Nash, M., Shardlow, C.E., Stemp, G., Thewlis, K., Ayrton, A., Jeffrey, P. Xenobiotica (2001) [Pubmed]
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