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
- ^ 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. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1574197.
- ^ 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.
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| GABAA agonists/PAMs |
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| GABAB agonists |
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| H1 inverse agonists |
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.)
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| α1-Adrenergic antagonists |
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| α2-Adrenergic agonists |
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| 5-HT2A antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors ( 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: Eplivanserin • Niaprazine • Pruvanserin • Volinanserin
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| Melatonin agonists |
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| Orexin antagonists |
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| Others |
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| Cholecystokinin |
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| CRH |
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| Galanin |
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| Ghrelin |
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| MCH |
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| Melanocortin |
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| Neuropeptide S |
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| Neuropeptide Y |
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| Neurotensin |
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| Opioid |
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| Orexin |
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| Oxytocin |
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| Tachykinin |
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Agonists: Substance P
Antagonists: Aprepitant • Befetupitant • Casopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
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| Vasopressin |
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