A α2-AR agonist
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Apraclonidine (hydrochloride)

Item No. 23904

Technical Information
Formal Name
2,6-dichloro-N1-(4,5-dihydro-1H-imidazol-2-yl)-1,4-benzenediamine, monohydrochloride
CAS Number
73218-79-8
Synonyms
  • AL0 2145
  • ALO 2145
Molecular Formula
C9H10Cl2N4 • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: Slightly SolubleMethanol: Slightly Soluble
SMILES
ClC1=C(NC2=NCCN2)C(Cl)=CC(N)=C1.Cl
InChi Code
InChI=1S/C9H10Cl2N4.ClH/c10-6-3-5(12)4-7(11)8(6)15-9-13-1-2-14-9;/h3-4H,1-2,12H2,(H2,13,14,15);1H
InChi Key
OTQYGBJVDRBCHC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Apraclonidine is an α2-adrenergic receptor (α2-AR) agonist and structural analog of clonidine (Item No. 15949).1 It binds to α2-ARs in calf cortex, rat kidney, and rat spleen with IC50 values of 0.9, 4.3, and 4.2 nM, respectively. Apraclonidine also binds to α2-ARs in rat cerebral cortex, pig submandibular gland and lung tissue, and in dog kidney membrane (Kds = 0.87, 5.28, 1.30, and 5.25 nM, respectively).2,3 It inhibits noradrenaline-stimulated contraction in guinea pig ileum and rabbit vas deferens (EC50s = 7.59 and 6.76 nM, respectively).4 Opthalmic formulations containing apraclonidine have been used to treat elevated intraocular pressure.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rouot, B.R., and Snyder, S.H. [3H]Para-amino-clonidine: A novel ligand which binds with high affinity to alpha-adrenergic receptors. Life Sci. 25(9), 769-774 (1979).

    2. Feller, D.J., and Bylund, D.B. Comparison of alpha-2 adrenergic receptors and their regulation in rodent and porcine species. J. Pharmacol. Exp. Ther. 228(2), 275-282 (1984).

    3. Evans, R.G., and Haynes, J.M. Characterization of binding sites for [3H]-idazoxan, [3H]-P-aminoclonidine and [3H]-rauwolscine in the kidney of the dog. Clin. Exp. Pharmacol. Physiol. 21(8), 649-658 (1994).

    4. Konno, F., Kusunoki, M., and Takayanagi, I. Receptor interactions of a series of imidazolines: Comparison of the alpha 2-adrenoceptors between the rabbit vas deferens and guinea pig ileum. Jpn. J. Pharmacol. 44(2), 171-178 (1987).