Stavudine (d4T)

- Overview
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    Background
    
    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]
    
    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.
- Properties
  - Alternative Name
    
    1-[(2R,5S)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4-dione
    
    CAS Number
    
    3056-17-5
    
    Molecular Formula
    
    C10H12N2O4
    
    Molecular Weight
    
    224.21
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥51.3 mg/mL in H2O; ≥8.4 mg/mL in DMSO; ≥9.72 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Stavudine (d4T)

Background

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