| Name | BRL 54443 |
| Description | BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values: 8.7 and 8.9, respectively). |
| Kinase Assay | In Vitro Radiometric PKD Kinase Assay: The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter. |
| In vitro | BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors. |
| In vivo | BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (8.68 mM)
DMSO : 43 mg/mL (186.7 mM)
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| Keywords | 5-HT Receptor | BRL 54443 | 5-hydroxytryptamine Receptor | Inhibitor | BRL-54443 | Serotonin Receptor | inhibit |
| 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 | Target-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Parkinson's Disease Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
