SB-408124

SB-408124
Identifiers

IUPAC name 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea
CAS Number	288150-92-5^Y
PubChem CID	4331799
IUPHAR/BPS	1704
ChemSpider	3536200^N
ECHA InfoCard	100.164.461
Chemical and physical data
Formula	C₁₉H₁₈F₂N₄O
Molar mass	356.368 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)^N Key:JTARFZSNUAGHRB-UHFFFAOYSA-N^N
^NY (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.^[1]^[2]

References

↑ 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. PMC 1574197 . PMID 14691055. doi:10.1038/sj.bjp.0705610.
↑ 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. PMID 18477704. doi:10.1152/ajpendo.90243.2008.

Hypnotics/sedatives (N05C)

GABA_A

Alcohols	2M2B Chloralodol Ethanol Alcohol 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 Doxefazepam Estazolam Flunitrazepam Flurazepam Flutoprazepam Haloxazolam Loprazolam Lormetazepam Midazolam Nimetazepam Nitrazepam Phenazepam 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
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 Pheniramine Promethazine Propiomazine
Antidepressants	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

Others

Signaling peptide/protein receptor modulators

Adiponectin

AdipoR₁	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon (–)-Arctigenin Arctiin Gramine Matairesinol Antagonists: Peptide: ADP-400
AdipoR₂	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon Deoxyschizandrin Parthenolide Syringing Taxifoliol Antagonists: Peptide: ADP-400

Angiotensin

Agonists: Angiotensin II
Angiotensin III
Angiotensin IV
Saralasin

Antagonists: Abitesartan
Azilsartan
Azilsartan medoxomil
Candesartan
Elisartan
Embusartan
Eprosartan
EXP-3174
Fimasartan
Forasartan
Irbesartan
Losartan
Milfasartan
Olmesartan
Olmesartan medoxomil
PD123319
Pomisartan
Pratosartan
Ripisartan
Saprisartan
Sparsentan
Tasosartan
Telmisartan
Valsartan
Zolasartan

Renin inhibitors: Aliskiren
Ciprokiren
Ditekiren
Enalkiren
Pepstatin
Remikiren
Terlakiren
Zankiren

Propeptides: Angiotensinogen
Angiotensin I

Bradykinin

Agonists: Bradykinin
Kallidin

Antagonists: FR-173657
Icatibant
LF22-0542

CGRP

Agonists: Amylin
CGRP
Pramlintide

Antagonists: BI 44370 TA
CGRP (8-37)
MK-3207
Olcegepant
Rimegepant
SB-268262
Telcagepant
Ubrogepant

Antibodies: Erenumab

Cholecystokinin

CCK_A	Agonists: Cholecystokinin Antagonists: Amiglumide Asperlicin Devazepide Dexloxiglumide Lintitript Lorglumide Loxiglumide Pranazepide Proglumide Tarazepide Tomoglumide
CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Pentagastrin (CCK-5) Antagonists: CI-988 (PD-134308) Itriglumide L-365,360 Netazepide Proglumide Spiroglumide
Unsorted	Antagonists: Nastorazepide

CRH

CRF₁	Agonists: Cortagine Corticorelin Corticotropin releasing hormone Sauvagine Stressin I Urocortin Antagonists: Antalarmin Astressin-B CP-154,526 Emicerfont Hypericin LWH-234 NBI-27914 Pexacerfont R-121919 TS-041 Verucerfont
CRF₂	Agonists: Corticorelin Corticotropin releasing hormone Sauvagine Urocortin Antagonists: Astressin-B

Cytokine

See here instead.

Endothelin

Agonists: Endothelin 1
Endothelin 2
Endothelin 3
IRL-1620

Antagonists: A-192621
ACT-132577
Ambrisentan
Atrasentan
Avosentan
Bosentan
BQ-123
BQ-788
Clazosentan
Darusentan
Edonentan
Enrasentan
Fandosentan
Feloprentan
Macitentan
Nebentan
Sitaxentan
Sparsentan
Tezosentan
Zibotentan

Galanin

GAL₁	Agonists: Galanin Galanin (1-15) Galanin-like peptide Galmic Galnon Antagonists: C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH-202596
GAL₂	Agonists: Galanin Galanin (1-15) Galanin (2-11) Galanin-like peptide Galmic Galnon J18 Antagonists: C7 Galantide (M15) M32 M35 M40 M871
GAL₃	Agonists: Galanin Galanin (1-15) Galmic Galnon Antagonists: C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299

Ghrelin/GHS

See here instead.

See here instead.

GHRH

See here instead.

GLP

GLP-1	Agonists: Albiglutide Dulaglutide Efpeglenatide Exenatide GLP-1 Langlenatide Liraglutide Lixisenatide Oxyntomodulin Semaglutide Taspoglutide
GLP-2	Agonists: Elsiglutide GLP-2 Teduglutide
Others	Propeptides: Preproglucagon Proglucagon

Glucagon

Agonists: Glucagon
Oxyntomodulin

Antagonists: Adomeglivant
L-168,049
LGD-6972

Propeptides: Preproglucagon
Proglucagon

GnRH

Antagonists: Peptide: Abarelix
Acyline
Cetrorelix
Degarelix
Detirelix
Ganirelix
Iturelix
Ozarelix
Prazarelix
Ramorelix
Teverelix (antarelix); Non-peptide: ASP-1707
Elagolix
KLH-2109 (OBE-2109)
Relugolix
Sufugolix

Gonadotropin

LH/CG	Agonists: Choriogonadotropin alfa Human chorionic gonadotropin Luteinizing hormone Lutropin alfa Menotropin (human menopausal gonadotropin)
FSH	Agonists: Corifollitropin alfa Follicle-stimulating hormone Follitropin alfa Follitropin beta Follitropin epsilon Menotropin (human menopausal gonadotropin) Urofollitropin Varfollitropin alfa NAMs: ADX-61623

Growth factor

See here instead.

Insulin

Antagonists: BMS-754807
S661
S961

Kinase inhibitors: Linsitinib

Antibodies: Xentuzumab (against IGF-1 and IGF-2)

Kisspeptin

Agonists: Kisspeptin
Kisspeptin-10

Antagonists: Kisspeptin-234

Leptin

Agonists: Leptin
Metreleptin

MCH

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0065 ATC-0175 GW-803430 NGD-4715 SNAP-7941 SNAP-94847
MCH₂	Agonists: Melanin concentrating hormone

Melanocortin

See here instead.

Neuropeptide FF

Agonists: Neuropeptide AF
Neuropeptide FF
Neuropeptide SF (RFRP-1)
Neuropeptide VF (RFRP-3)

Antagonists: BIBP-3226
RF9

Neuropeptide S

Agonists: Neuropeptide S

Antagonists: ML-154
SHA-68

Neuropeptide Y

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBO-3304 BIBP-3226 BVD-10 GR-231118 PD-160170
Y₂	Agonists: 2-Thiouridine 5'-triphosphate Neuropeptide Y Neuropeptide Y (13-36) Peptide YY Peptide YY (3-36) Antagonists: BIIE-0246 JNJ-5207787 SF-11
Y₄	Agonists: GR-231118 Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49
Y₅	Agonists: BWX-46 Neuropeptide Y Peptide YY Antagonists: CGP-71683 FMS-586 L-152,804 Lu AA-33810 MK-0557 NTNCB Velneperit (S-2367)

Neurotensin

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: Meclinertant SR-142948
NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142948

Opioid

See here instead.

Orexin

OX₁	Agonists: Orexin (A, B) Antagonists: ACT-335827 ACT-462206 Almorexant Filorexant Lemborexant SB-334867 SB-408124 SB-649868 Suvorexant TCS-1102
OX₂	Agonists: Orexin (A, B) SB-668875 Antagonists: ACT-335827 ACT-462206 Almorexant EMPA Filorexant JNJ-10397049 Lemborexant MK-1064 SB-649868 Seltorexant Suvorexant TCS-1102 TCS-OX2-29

Oxytocin

See here instead.

Prolactin

Agonists: Growth hormone
Human placental lactogen
Placental growth hormone (growth hormone variant)
Prolactin
S179D-hPRL
Somatotropin

Antagonists: Δ1–9-G129R-hPRL
Δ1–14-G129R-hPRL
G120K-hGH
G129R-hPRL

Prolactin modulators: Prolactin inhibitors: D₂ receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D₂ receptor antagonists (e.g., domperidone, metoclopramide, risperidone)
Estrogens (e.g., estradiol)
Progestogens (e.g., progesterone)

PTH

Agonists: Abaloparatide
Parathyroid hormone
Parathyroid hormone-related protein (PTHrP)
Semparatide
Teriparatide

Relaxin

Somatostatin

See here instead.

Tachykinin

See here instead.

TRH

Agonists: Azetirelin
Fertirelin
Montirelin
Orotirelin
Posatirelin
Protirelin
Rovatirelin
Taltirelin
TRH (TRF)

TSH

Agonists: Thyrotropin alfa
TSH (thyrotropin)

Vasopressin

See here instead.

VIP/PACAP

VIPR₁	Agonists: Peptide: Bay 55-9837 LBT-3393 PACAP VIP
VIPR₂	Agonists: Peptide: LBT-3627 PACAP VIP
PAC₁	Agonists: PACAP PACAP (1-27) PACAP (1-38) Antagonists: PACAP (6-38)
Unsorted	PHI PHM PHV

Others

Endogenous: Adrenomedullin
Apelin
Asprosin
Bombesin
Calcitonin
Carnosine
CART
CLIP
DSIP
Enteroglucagon
Formyl peptide
GALP
GIP
GRP
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin)
Kininogens
Motilin
Natriuretic peptides (ANP, BNP, CNP, urodilatin)
Nesfatin-1
Neuromedin B
Neuromedin N
Neuromedin S
Neuromedin U
Obestatin
Osteocalcin
Resistin
Secretin
Thymopoietin
Thymosins
Thymulin
Urotensin-II
VGF

Exogenous: Lifitegrast (LFA-1 antagonist)

See also: Receptor/signaling modulators

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