| Name | GSK163090 |
| Description | GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3). |
| In vitro | GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyper locomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated a moderate functional antagonism of the phenylephrine-induced contraction of rabbit aorta (pIC50: 6.9). |
| In vivo | The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokinetic profile in rats and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.41 mM), Sonication is recommended.
DMSO : 14.29 mg/mL (34.39 mM), Sonication is recommended.
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| Keywords | SerT | Serotonin Receptor | P-glycoprotein | Inhibitor | inhibit | GSK-163090 | GSK163090 | GSK 163090 | DopamineReceptor | Dopamine Receptor | Dopamine | anxiolytic | antidepressant | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1D | 5-HT1B | 5-HT1A | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | Cefaclor monohydrate | Hexamethonium Bromide | Octopamine hydrochloride | 1,8-Cineole | L-DOPA | Creatine | Oxolinic acid | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
