Stereochemistry | ACHIRAL |
Molecular Formula | C10H16N2O |
Molecular Weight | 180.2468 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C1CC1C(NC2=NCCO2)C3CC3
InChI
InChIKey=CQXADFVORZEARL-UHFFFAOYSA-N
InChI=1S/C10H16N2O/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10/h7-9H,1-6H2,(H,11,12)
Molecular Formula | C10H16N2O |
Molecular Weight | 180.2468 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Rilmenidine (brand names Albarel, Hyperium, Iterium and Tenaxum) is an imidazoline derivative used for the treatment of hypertension. Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Rilmenidine is as effective in monotherapy as all other first line classes of drugs, including diuretics, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tolerated and can be taken in combination for greater efficacy. Sedation and dry mouth are not prominent side effects and withdrawal hypertension is not seen when treatment is stopped abruptly. In addition to a reduction in blood pressure, Rilmenidine has been shown to improve glucose tolerance, lipid risk factors, and insulin sensitivity.
CNS Activity
Approval Year
Cmax
T1/2
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
PubMed
Patents
Sample Use Guides
The cytotoxic activity of rilmenidine and doxorubicin on K562 cells was measured using the MTT assay. After treatment in 96-well plates, MTT solution (3-(4,5-dimethylthiazol-2-yl)-2,5-dyphenyl tetrazolium bromide) (20 μL/well) was added to each well. Sampleswere incubated for a further 4 h, followed by the addition of 100 μl of 10% SDS. Absorbance at 570 nmwasmeasured the next day.