An imidazoline I1 and α2A-adrenergic receptor agonist
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Moxonidine

Item No. 25639

Technical Information
Formal Name
4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamine
CAS Number
75438-57-2
Synonyms
  • LY326869
Molecular Formula
C9H12ClN5O
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 2 mg/ml
λmax
222, 256 nm
SMILES
CC1=NC(Cl)=C(NC2=NCCN2)C(OC)=N1
InChi Code
InChI=1S/C9H12ClN5O/c1-5-13-7(10)6(8(14-5)16-2)15-9-11-3-4-12-9/h3-4H2,1-2H3,(H2,11,12,15)
InChi Key
WPNJAUFVNXKLIM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Moxonidine is an imidazoline 1 (I1) receptor agonist (Ki = 56 nM in a radioligand binding assay).1 It is also an agonist of the α2A-adrenergic receptor (α2A-AR; Ki = 150 nM in a radioligand binding assay). It is selective for I1 and α2A-AR receptors over α1-, α2B, and α2C-ARs (Kis = >30,000, 1,000, and 2,000 nM, respectively). Moxonidine decreases mean arterial pressure in spontaneously hypertensive rats when administered at a dose of 0.2 nmol injected into the rostral ventrolateral medulla oblongata (RVLM).2 It also reduces blood pressure in cynomolgus monkeys when administered at a dose of 167 µg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Munk, S.A., Lai, R.K., Burke, J.E., et alSynthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J. Med. Chem. 39(6), 1193-1195 (1996).

    2. Ernsberger, P., Haxhiu, M.A., Graff, L.M., et alA novel mechanism of action for hypertension control: moxonidine as a selective I1-imidazoline agonist. Cardiovasc. Drugs Ther. 8(Suppl 1), 27-41 (1994).