SB-408,124

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SB-408,124
Systematic (IUPAC) name
N-(6,8-Difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]urea
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 288150-92-5
ATC code  ?
Chemical data
Formula C19H18F2N4O 
Mol. mass 356.368 g/mol
 YesY (what is this?)  (verify)

SB-408,124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70x selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334,867. It is used in scientific research into the function of orexinergic neurons in the body.[1][2]

[edit] References

  1. ^ Langmead, CJ; Jerman, JC; Brough, SJ; Scott, C; Porter, RA; Herdon, HJ (2004). "Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor". British Journal of Pharmacology 141 (2): 340–6. doi:10.1038/sj.bjp.0705610. PMC 1574197. PMID 14691055. 
  2. ^ Peng, HY; Chang, HM; Chang, SY; Tung, KC; Lee, SD; Chou, D; Lai, CY; Chiu, CH et al. (2008). "Orexin-A modulates glutamatergic NMDA-dependent spinal reflex potentiation via inhibition of NR2B subunit". American journal of physiology. Endocrinology and metabolism 295 (1): E117–29. doi:10.1152/ajpendo.90243.2008. PMID 18477704. 
GABAA
agonists/PAMs
Alcohols: 2M2B • Chloralodol • Ethanol (Alcohol) • Ethchlorvynol • Methylpentynol • Trichloroethanol
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Carbamates: Carisoprodol • Ethinamate • Hexapropymate • Meprobamate • Methocarbamol • Procymate • Tybamate
Neuroactive Steroids: Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Eltanolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • Org 21465 • Tetrahydrodeoxycorticosterone
Nonbenzodiazepines: CL-218,872 • Eszopiclone • Indiplon • JM-1232 • Lirequinil • Necopidem • Pazinaclone • ROD-188 • Saripidem • Suproclone • Suriclone • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiclone
Phenols: Fospropofol • Propofol
Piperidinediones: Glutethimide • Methyprylon • Pyrithyldione • Piperidione
Quinazolinones: Afloqualone • Cloroqualone • Diproqualone • Etaqualone • Mebroqualone • Mecloqualone • Methaqualone • Methylmethaqualone • Nitromethaqualone • SL-164
Volatiles/gases: • Acetophenone • Acetylglycinamide chloral hydrate • Centalun • Chloral hydrate • Paraldehyde
Others: Bromide (Lithium bromide, Potassium bromide, Sodium bromide) • Chloralose • Clomethiazole • Dichloralphenazone • Etomidate • Gaboxadol • Loreclezole • Metomidate • Org 25435 • Petrichloral • Sulfonmethane • Triclofos • Valerenic acid (Valerian)
GABAB
agonists
1,4-Butanediol • Aceburic acid • GABOB • GHB (Sodium oxybate) • GBL • GVL
H1 inverse
agonists
α1-Adrenergic
antagonists
α2-Adrenergic
agonists
5-HT2A
antagonists
Melatonin
agonists
Orexin
antagonists
Almorexant • SB-334,867 • SB-408,124 • SB-649,868 • Suvorexant • TCS-OX2-29
Others
Cholecystokinin
CRH
Galanin
Ghrelin
GnRH
MCH
Melanocortin
Neuropeptide S
Neuropeptide Y
Neurotensin
Orexin
Oxytocin
Tachykinin
Vasopressin
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