ROD-188 is a sedative drug structurally derived from the GABAA antagonist bicuculline. Unlike bicuculline, ROD-188 acts as an agonist at GABAA receptors, being a positive allosteric modulator acting at a novel binding site distinct from those of benzodiazepines, barbiturates or muscimol, with its strongest effect produced at the α6β2γ2 subtype of the GABAA receptor.[1] ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.[2]
[edit] See also
[edit] References
- ^ Thomet U, Baur R, Razet R, Dodd RH, Furtmüller R, Sieghart W, Sigel E. A novel positive allosteric modulator of the GABA(A) receptor: the action of (+)-ROD188. British Journal of Pharmacology. 2000 Oct;131(4):843-50. PMID 11030736
- ^ Sigel E, Baur R, Furtmueller R, Razet R, Dodd RH, Sieghart W. Differential cross talk of ROD compounds with the benzodiazepine binding site. Molecular Pharmacology. 2001 Jun;59(6):1470-7. PMID 11353808
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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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