Lofexidine

SKU: orb1300016

Description

Lofexidine is a selective α2-adrenergic receptor agonist used in research to mitigate symptoms of opioid withdrawal. It is applied in both in vivo and in vitro studies within neuropharmacology and addiction research to investigate autonomic regulation and withdrawal mechanisms.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 31036-80-3
• MW: 259.13
• Purity: 99.08% (May vary between batches)
• Formula: C₁₁H₁₂Cl₂N₂O
• SMILES: CC(Oc1c(Cl)cccc1Cl)C1=NCCN1
• Target: Adrenergic Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.72 mM);DMSO:62.5 mg/mL (241.19 mM)

Bioactivity

• In Vivo:
  Lofexidine significantly decreased SOWS scores compared to placebo and demonstrated better retention rates in participants undergoing opioid withdrawal. Lofexidine potentially offers a useful non-opioid alternative to treat opioid withdrawal symptoms.
• Animal Research:
  8-day, randomized, double-blind, placebo-controlled, parallel-group study in 264 patients dependent on short-acting opioids evaluated the efficacy of lofexidine hydrochloride in reducing withdrawal symptoms in patients undergoing opioid withdrawal. The primary efficacy measures were SOWS-Gossop on Day 3 and time-to-dropout. Secondary endpoints included the proportion of participants who were completers; area under the 5-day SOWS-Gossop - time curve (i.e., AUC1-5), and daily mean SOWS-Gossop, OOWS-Handelsman, MCGI (subject and rater), and VAS-E scores. Participants received lofexidine HCl 3.2mg daily in four divided doses or matching placebo on Days 1-5, followed by 2days of placebo.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

α2 receptor, inhibit, Inhibitor, Lofexidine, Adrenergic Receptor, AdrenergicReceptor, Beta Receptor

Compound Identifiers

PubChem CID

30668