An antihypertensive agent
Related Products
Alternative(s)
32879Rilmenidine
Labeled Version(s)
31691Rilmenidine-d4
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Rilmenidine (hemifumarate)

Item No. 16988

Technical Information
Formal Name
N-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine, 2E-butenedioate (2:1)
CAS Number
207572-68-7
Synonyms
  • Oxaminozoline
  • S 3341
Molecular Formula
C10H16N2O • 1/2C4H4O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 3 mg/mlDMSO: 3 mg/mlEthanol: 10 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
SMILES
OC(/C=C/C(O)=O)=O.C1(NC(C2CC2)C3CC3)=NCCO1.C4(NC(C5CC5)C6CC6)=NCCO4
InChi Code
InChI=1S/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12);1-2H,(H,5,6)(H,7,8)/b;;2-1+
InChi Key
LZFATBMLSYHRTC-WXXKFALUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Rilmenidine is an antihypertensive agent.1 It binds to imidazole receptors in bovine rostral ventrolateral medulla homogenates (Ki = 6.1 nM), as well as α2-adrenergic receptors in bovine prefrontal cortex homogenates (Ki = 87 nM). Rilmenidine induces hypotension and bradycardia in anesthetized rats (ED50s = 0.25 and 0.35 mg/kg, respectively). It also reduces mean arterial pressure and renal sympathetic nerve activity in a rabbit model of renal hypertension induced by a renal artery clip when administered at a dose of 2.5 mg/kg.2 Rilmenidine (1 µM) increases levels of LC3-II, a marker of autophagy, in PC12 cells.3 Formulations containing rilmenidine have been used in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gomez, R.E., Ernsbarger, P., Feinland, G., et alRilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 area. Eur. J. Pharmacol. 195(2), 181-191 (1991).

    2. Burke, S.L., Evans, R.G., and Head, G.A. Effects of chronic sympatho-inhibition on renal excretory function in renovascular hypertension. J. Hypertens. 29(5), 945-952 (2011).

    3. Williams, A., Sarkar, S., Cuddon, P., et alNovel targets for Huntington’s disease in an mTOR-independent autophagy pathway. Nat. Chem. Biol. 4(5), 295-305 (2008).