An α2-adrenergic receptor agonist
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Lofexidine (hydrochloride)

Item No. 15989

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole, monohydrochloride
CAS Number
21498-08-8
Molecular Formula
C11H12Cl2N2O • HCl
Formula Weight
295.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
ClC1=CC=CC(Cl)=C1OC(C)C2=NCCN2.Cl
InChi Code
InChI=1S/C11H12Cl2N2O.ClH/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13;/h2-4,7H,5-6H2,1H3,(H,14,15);1H
InChi Key
DWWHMKBNNNZGHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    250 mg

    $44

    Add

    500 mg

    $71

    Add

    1 g

    $105

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    Product Description

    Lofexidine is an α2-adrenergic receptor agonist (Kd = 7.6 nM for rat cerebral cortex membranes) that has transient antihypertensive effects.1,2 It is used in managing opioid withdrawal symptoms during detoxification from heroin (Item No. 9001543) and methadone.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jarrott, B., Louis, W.J., and Summers, R.J. Characterization of central α-adrenoceptors using 3H-clonidine and its derivatives. Chest 83(2 Suppl), 339-340 (1983).

    2. Bennett, D.A., and Lal, H. Discriminative stimuli produced by clonidine: An investigation of the possible relationship to adrenoceptor stimulation and hypotension. J. Pharmacol. Exp. Ther. 223(3), 642-648 (1982).

    3. Ling, W., Mooney, L., Zhao, M., et al. Selective review and commentary on emerging pharmacotherapies for opioid addiction. Subst. Abuse Rehabil. 2, 181-188 (2011).

    4. Gerra, G., Zaimovic, A., Giusti, F., et al. Lofexidine versus clonidine in rapid opiate detoxification. J. Subst. Abuse Treat. 21(1), 11-17 (2001).