| Name | AZD-6280 |
| Description | AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder. |
| Animal Research | Two PET studies, using high-resolution research tomography (HRRT) and the radioligand [11C]flumazenil, were performed in 12 subjects at baseline and after administration of single oral doses of AZD7325 (0.2 to 30 mg) and AZD6280 (5 to 40 mg). PET images were analyzed using a simplified reference tissue model, and regional binding potentials (BPND) were obtained. The relationship between plasma concentration of AZD7325 or AZD6280 and GABAA receptor occupancy was described by hyperbolic function, and K i,plasma (plasma concentration required for 50% receptor occupancy) was estimated. Assessments of safety and tolerability included recording of adverse events, vital signs, electrocardiogram, and laboratory tests[1]. |
| In vivo | The [11C]flumazenil binding was reduced in a dose-dependent, saturable manner by AZD6280. Maximum receptor occupancy could be reached for AZD6280 without causing sedation or cognitive impairment. The K i,plasma estimates for AZD6280 was 440 nmol/l[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 25 mg/mL (68.23 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.46 mM), Sonication is recommended.
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| Keywords | γ-Aminobutyric acid Receptor | Inhibitor | inhibit | Gamma-aminobutyric acid Receptor | GABAReceptor | GABAA | GABA Receptor | AZD-6280 | AZD6280 | AZD 6280 |
| Inhibitors Related | Valproic acid sodium salt | p-Hydroxybenzaldehyde | Urethane | Baicalin | Penicillin G sodium salt | Valproic Acid | Methyl eugenol | (-)-α-Pinene | Nipecotic acid | Methionine | Dihydromyricetin | Isoflurane |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Clinical Compound Library | Neurotransmitter Receptor Compound Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
