SB-408124 Hydrochloride |
| Catalog No.GC16540 |
A potent orexin 1 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1431697-90-3
Sample solution is provided at 25 µL, 10mM.
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SB-408124 Hydrochloride is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.IC50 Value: 57 nM(Ki)Target: OX1 Receptorin vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.in vivo: SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).
References:
[1]. Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340.
[2]. Morairty SR, et al. Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone.PLoS One. 2012;7(7):e39131. Epub 2012 Jul 2.
[3]. Melis MR, et al. Neuroendocrine regulatory peptide-1 and neuroendocrine regulatory peptide-2 influence differentially feeding and penile erection in male rats: sites of action in the brain.Regul Pept. 2012 Aug 20;177(1-3):46-52. Epub 2012 May 2.
[4]. Assisi L, et al. Expression and role of receptor 1 for orexins in seminiferous tubules of rat testis.Cell Tissue Res. 2012 Jun;348(3):601-7. Epub 2012 Mar 28.
[5]. Kis GK, et al.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. Epub 2012 Feb 16.
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