SB-408124 - Misplaced Pages

(Redirected from SB-408,124) Chemical compound

Pharmaceutical compound

SB-408124
Identifiers

IUPAC name 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-urea
CAS Number	288150-92-5
PubChem CID	4331799
IUPHAR/BPS	1704
ChemSpider	3536200
CompTox Dashboard (EPA)	DTXSID20402022
ECHA InfoCard	100.164.461
Chemical and physical data
Formula	C₁₉H₁₈F₂N₄O
Molar mass	356.377 g·mol
3D model (JSmol)	Interactive image
SMILES c3cc(N(C)C)ccc3NC(=O)Nc1cc(C)nc2c1cc(F)cc2F
InChI InChI=1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26) Key:JTARFZSNUAGHRB-UHFFFAOYSA-N
(what is this?) (verify)

SB-408124 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-334867. It is used in scientific research into the function of orexinergic neurons in the body.

References

Langmead CJ, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ (January 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.
Peng HY, Chang HM, Chang SY, Tung KC, Lee SD, Chou D, et al. (July 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. S2CID 587272.

Hypnotics/sedatives (N05C)

GABA_A

Alcohols	2M2B Chloralodol Ethanol (alcohol) Diethylpropanediol Ethchlorvynol Methylpentynol Trichloroethanol
Barbiturates	Allobarbital Amobarbital Aprobarbital Barbital Butabarbital Butobarbital Cyclobarbital Ethallobarbital Heptabarb Hexobarbital Mephobarbital Methohexital Narcobarbital Pentobarbital Phenallymal Phenobarbital Propylbarbital Proxibarbal Reposal Secobarbital Talbutal Thiamylal Thiopental Thiotetrabarbital Vinbarbital Vinylbital
Benzodiazepines	Brotizolam Cinolazepam Climazolam Clonazolam Doxefazepam Estazolam Flubromazolam Flunitrazolam Flunitrazepam Flurazepam Flutemazepam Flutoprazepam Loprazolam Lormetazepam Midazolam Nimetazepam Nitemazepam Nitrazepam Nitrazolam Quazepam Temazepam Triazolam
Carbamates	Carisoprodol Emylcamate Ethinamate Hexapropymate Meprobamate Methocarbamol Phenprobamate Procymate Tybamate
Imidazoles	Etomidate Metomidate Propoxate
Monoureides	Acecarbromal Apronal (apronalide) Bromisoval Capuride Carbromal Ectylurea
Neuroactive steroids	Acebrochol Allopregnanolone Alphadolone Alphaxolone Eltanolone Hydroxydione Minaxolone Progesterone
Nonbenzodiazepines	Eszopiclone Indiplon Lirequinil Necopidem Pazinaclone Saripidem Suproclone Suriclone Zaleplon Zolpidem Zopiclone
Phenols	Propofol
Piperidinediones	Glutethimide Methyprylon Pyrithyldione Piperidione
Quinazolinones	Afloqualone Cloroqualone Diproqualone Etaqualone Mebroqualone Mecloqualone Methaqualone Methylmethaqualone Nitromethaqualone SL-164
Others	Acetophenone Acetylglycinamide chloral hydrate Bromide compounds Lithium bromide Potassium bromide Sodium bromide Centalun Chloral betaine Chloral hydrate Chloralose Clomethiazole Dichloralphenazone Gaboxadol Kavalactones Loreclezole Paraldehyde Petrichloral Sulfonylalkanes Sulfonmethane (sulfonal) Tetronal Trional Triclofos Sesquiterpene Isovaleramide Isovaleric acid Valerenic acid

GABA_B

H₁

Antihistamines	Captodiame Cyproheptadine Diphenhydramine Doxylamine Hydroxyzine Methapyrilene Perlapine Pheniramine Promethazine Propiomazine
Antidepressants	Serotonin antagonists and reuptake inhibitors Etoperidone Nefazodone Trazodone Tricyclic antidepressants Amitriptyline Doxepin Trimipramine, etc. Tetracyclic antidepressants Mianserin Mirtazapine, etc.
Antipsychotics	Typical antipsychotics Chlorpromazine Thioridazine, etc. Atypical antipsychotics Olanzapine Quetiapine Risperidone, etc.

α₂-Adrenergic

5-HT_2A

Antidepressants	Trazodone Tricyclic antidepressants Amitriptyline Doxepin Trimipramine, etc. Tetracyclic antidepressants Mianserin Mirtazapine, etc.
Antipsychotics	Typical antipsychotics Chlorpromazine Thioridazine, etc. Atypical antipsychotics Olanzapine Quetiapine Risperidone, etc.
Others	Niaprazine

Melatonin

Orexin

α₂δ VDCC

Others

v t e Orexin receptor modulators
OX₁	Agonists: AEX-5 AEX-19 AEX-24 Orexin (A, B) Antagonists: ACT-335827 ACT-462206 Almorexant AZD-4041 C4X-3256 (INDV-2000) CR-5542 CVN-766 Daridorexant Fazamorexant (YZJ-1139) Filorexant GSK-649868 (SB-649868) Lemborexant Nivasorexant (ACT-539313) RTIOX-276 SB-334867 SB-408124 Suvorexant TCS-1102 Tebideutorexant (JNJ-61393215) Vornorexant (ORN-0829, TS-142)
OX₂	Agonists: AEX-19 ALKS-2680 Danavorexton (TAK-925) E-2086 Firazorexton (TAK-994) Orexin (A, B) Oveporexton SB-668875 Suntinorexton (TAK-861) Antagonists: ACT-335827 ACT-462206 Almorexant Daridorexant EMPA Fazamorexant (YZJ-1139) Filorexant GSK-649868 (SB-649868) JNJ-10397049 Lemborexant MK-1064 MK-3697 MK-8133 Seltorexant Suvorexant TCS-1102 TCS-OX2-29 Vornorexant (ORN-0829, TS-142)

Orexin receptor modulators

OX₁

Agonists: AEX-5
AEX-19
AEX-24
Orexin (A, B)

OX₂

This sedative-related article is a stub. You can help Misplaced Pages by expanding it.

Categories: