3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol
BRL-54443
CAS: 57477-39-1
Molecular Formula: C14H18N2O
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol - Names and Identifiers
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol - Physico-chemical Properties
| Molecular Formula | C14H18N2O |
| Molar Mass | 230.31 |
| Density | 1.196 |
| Boling Point | 431.5±45.0 °C(Predicted) |
| Solubility | H2O: 50mg/mL |
| Appearance | solid |
| Color | white |
| pKa | 10.08±0.40(Predicted) |
| Storage Condition | Inert atmosphere,2-8°C |
| Use | A potent agonist at SR-1E and SR-1F. |
| In vitro study | Despite its low affinity for other receptors [5-HT 1A (63 nM), 5-HT 1B (126 nM), 5-HT 1D (63 nM), 5-HT 2A (1259 nM), 5-HT 2B (100 nM), 5-HT 2C (316 nM), 5-HT 6 (>10,000 nM), 5-HT 7 (>10,000 nM), D 2 (501 nM), D 3 (631 nM), and α 1B -adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT 1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT 1E receptors and potently inhibits forskolin-dependent cAMP production (IC 50 =14 nM). BRL 54443 also induces contraction (-log EC 50 =6.52). |
| In vivo study | Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats. |
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol - Introduction
BRL-54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi 8.7 and 9.25, respectively, and has a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
Last Update：2022-10-16 17:41:43
3-(1-Methyl-4-piperidinyl)-1H-indol-5-ol - Reference Information
| introduction | 3-(1-methyl-4-piperidinyl)-1H-indole-5-ol is a BRL-54443 that selectively agonists 5-HT1E and 5-HT1F serotonin receptor subtypes. Its preparation has attracted more and more attention from medical workers. |
| biological activity | BRL 54443 is a 5-HT1E/1F receptor agonist, Ki is 1.1 nM and 0.7 nM respectively, which is more than 30 times higher than other 5-HT and dopamine receptors. |
| target | 5-HT 1E Receptor 1.1 nM (Ki) 5-HT 1F Receptor 0.7 nM (Ki) 5-HT 1A Receptor 63 nM (Ki) 5-HT 1B Receptor 126 nM (Ki) 5-HT 1D Receptor 63 nM (Ki) 5-HT 2A Receptor 1259 nM (Ki) 5-HT 2B Receptor 100 nM (Ki) 5-HT 2C Receptor 316 nM (Ki) 5-HT 6 Receptor >10,000 nM (Ki) 5-HT 7 Receptor >10,000 nM (Ki) |
| in vitro study | Despite its low affinity for other receptors [5-HT 1A (63 nm), 5-HT 1B (126 nm), 5-HT 1D (63 nm), 5-HT 2A (1259 nm), 5-HT 2B (100 nM), 5-HT 2C (316 nM), 5-HT 6 (>10,000 nM), 5-HT 7 (>10,000 nM), D 2 (501 nM), D 3 (631 nM), and α 1B -adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT 1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT 1E receptors and potently inhibits forskolin-dependent cAMP production (IC 50=14 nM). BRL 54443 also induces contraction (-log EC 50=6.52). |
| in vivo study | Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats. |
Last Update：2024-04-09 21:54:55
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CAS: 57477-39-1
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CAS: 57477-39-1
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Mobile: 18021002903
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