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Cat. No. Name Size Price Add Cart
KI0774Rilmenidine50 mg$729

Chemical Characteristic

Product NameRilmenidine
SynonymsHyperium, Iterium, Tenaxum, S 3341
CAS No.54187-04-1
Molecular Weight 180.25
FormulaC10H16N2O
Chemical Structure

Biological activities

Rilmenidine is an imidazoline α2-adrenoceptor agonist. Rilmenidine inhibits noradrenaline-induced platelet aggregation with an IC50 of 12.7 µM.[1] Rilmenidine has high affinity for imidazoline I1 receptor with a Ki of 52 nM. In the untreated cells and ns-siRNA transfected cells, administration of rilmenidine at the dose of 100 nM for 15 minutes increases ERK phosphorylation to about 3 fold compared with vehicle control.[2] Rilmenidine at the dose of 1 µM inhibits isoproterenolstimulated cAMP accumulation in rabbit iris-ciliary bodies by 43%. Rilmenidine induces large increases in [Ca2+] in rabbit nonpigmented ciliary epithelial cells.[3] Rilmenidine prevents the firing of locus ceruleus and dorsal raphe neurons.[4] Rilmenidine which is microinjected bilaterally into the C1 area of the rostral ventrolateral medulla (RVL), but not nucleus tractus solitarii (NTS) nor caudal ventrolateral medulla (CVL), causes dose-dependent falls in arterial pressure and heart rate at doses an order of magnitude less than required systemically.[5] Rilmenidine administration improves the signs of disease in a Huntington's disease mouse model. Rilmenidine decreases levels of the mutant huntingtin fragment. Rilmenidine induces autophagy in mice and in primary neuronal culture.[6]

Protocols

In vivo: Rilmenidine is obtained in the form of rilmenidine hemifumarate. Rilmenidine hemifumarate is prepared as a stock solution of 10 mg/mL in 20% ethanol and is diluted on the day of experiment to 1 mg/mL in 0.15 m NaCl, 5% Tween-20 and 5% PEG 400 immediately before injection.[6]

References

[1] Pinthong D, et al. The effects of imidazoline agents on the aggregation of human platelets. J Pharm Pharmacol. 2004, 56(2): 213-220. 閵嗏偓閵嗏偓
[2] Li F, et al. Comparison of agmatine with moxonidine and rilmenidine in morphine dependence in vitro: role of imidazoline I(1) receptors. Eur J Pharmacol. 2009, 612(1-3): 1-8. 閵嗏偓閵嗏偓
[3] Chu TC, et al. Rilmenidine-induced ocular hypotension: role of imidazoline1 and alpha 2 receptors. Curr Eye Res. 1996, 15(9): 943-950. 閵嗏偓閵嗏偓
[4] Dresse A, et al. Action of rilmenidine on locus ceruleus and dorsal raphe cells in vivo and in vitro. Am J Cardiol. 1988, 61(7): 32D-34D. 閵嗏偓閵嗏偓
[5] Gomez RE, et al. Rilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 area. Eur J Pharmacol. 1991, 195(2): 181-191. 閵嗏偓閵嗏偓
[6] Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010, 19(11): 2144-2153. 閵嗏偓閵嗏偓

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