| Name | Temanogrel |
| Description | Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM). |
| In vitro | Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis (IC50: 13±7 nM) [1][3]. |
| In vivo | Plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6, and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h, and 2.25 h after the start of treatment in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment [3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 125 mg/mL (286.37 mM), Sonication is recommended.
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| Keywords | inhibit | Serotonin Receptor | 5-HT Receptor | Inhibitor | 5-hydroxytryptamine Receptor | APD 791 | Temanogrel | APD-791 |
| Inhibitors Related | Serotonin hydrochloride | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Mirtazapine | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
