TCS-OX2-29 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX2, with an IC50 of 40nM and selectivity of around 250x for OX2 over OX1 receptors.[1] Orexin antagonists are expected to be useful for the treatment of insomnia, with subtype-selective antagonists such as TCS-OX2-29 potentially offering more specificity of action compared to non-selective orexin antagonists like almorexant.[2]
References [edit]
- ^ Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorganic and Medicinal Chemistry Letters. 2003 Dec 15;13(24):4497-9. PMID 14643355
- ^ Roecker AJ, Coleman PJ. Orexin receptor antagonists: medicinal chemistry and therapeutic potential. Current Topics in Medicinal Chemistry. 2008;8(11):977-87. PMID 18673167
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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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