Stavudine (d4T)
SB-271046 is a potent, selective and orally active antagonist of 5-HT6 receptor (pKi = 8.9 in HeLa cell in vitro)
5-HT receptor is a G-protein coupled receptor for 5-hydroxytryptamine (serotonin) that found in nerve systems. It also functions as receptor for various alkaloids and psychoactive substances.
In native brain tissue, SB-271046 exhibits high affinity for human recombinant 5-HT6 receptors and 5-HT6 receptors. SB-271046 has a 200 fold greater selectivity over all other 5-HT receptors subtypes tested. [1]
In rat MEST (maximal electroshock seizure threshold) test, SB-271046 increases the seizure threshold over a wide range of dose with a minimum effective dose of 40.1 mg kg71 p.o. and maximum effect at 4 h post-dose. [1] In rat Morris water maze that measuring behavior acquisition and retention, galanthamine and SB-271046 combined treatment reverses the scopolamine- or MK-801-induced learning impairments. [2]
References:
1. Routledge C, Bromidge SM, Moss SF et al. Characterization of SB-271046: a potent, selective and orally active 5-HT (6) receptor antagonist. Br J Pharmacol. 2000 Aug; 130(7):1606-12.
2. Marcos B, Chuang TT, Gil-Bea FJ, Ramirez MJ. Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat. Br J Pharmacol. 2008 Oct;155(3):434-40.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 224.21 |
| Cas No. | 3056-17-5 |
| Formula | C10H12N2O4 |
| Solubility | ≥51.3 mg/mL in H2O; ≥8.4 mg/mL in DMSO; ≥9.72 mg/mL in EtOH with ultrasonic |
| Chemical Name | 1-[(2R,5S)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4-dione |
| SDF | Download SDF |
| Canonical SMILES | CC1=CN(C(=O)NC1=O)C2C=CC(O2)CO |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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Chemical structure
