SB408124

Uses

SB 408124 is a novel OX-1 antagonist.

Definition

ChEBI: 1-(6,8-difluoro-2-methyl-4-quinolinyl)-3-[4-(dimethylamino)phenyl]urea is a member of quinolines and an organohalogen compound.

Biological Activity

Selective non-peptide orexin OX 1 receptor antagonist (K b values are 21.7 and 1405 nM for human OX 1 and OX 2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo .

in vivo

IC 50

OX₁ Receptor: 57 nM (Ki, in whole cell ); OX₁ Receptor: 27 nM (Ki, in cell membrane)

storage

Store at RT

References

[1] langmead cj1, jerman jc, brough sj, scott c, porter ra, herdon hj.characterisation of the binding of [3h]-sb-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. br j pharmacol. 2004 jan;141(2):340-6.
[2] woldan-tambor a1, biegańska k, wiktorowska-owczarek a, zawilska jb. activation of orexin/hypocretin type 1 receptors stimulates camp synthesis in primary cultures of rat astrocytes. pharmacol rep. 2011;63(3):717-23.
[3] kis gk1, molnár ah, daruka l, gardi j, rákosi k, lászló f, lászló fa, varga c.the osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. pflugers arch. 2012 apr;463(4):531-6.