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.
- ^ 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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GnRH |
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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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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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