货号 | 16988-1mg |
描述 | Rilmenidine is a centrally acting antihypertensive agent that has been shown to lower arterial pressure in various animal models by inhibiting the tonic activity of sympathoexcitatory neurons in the rostral ventrolateral medulla.1 Rilmenidine targets the nonadrenergic imidazoline-binding site I1 receptor with a Ki value of 7.1 nM and demonstrates weaker affinity for the I2 receptor with a Ki value of 5.2 µM.2,3 It can also act as an agonist of α2-adrenergic receptors, but demonstrates ~30-fold greater selectivity for I1 receptors compared to α2-adrenergic receptors.4 Rilmenidine is reported to induce autophagy as evidenced by a ~350% increase in LC3-II levels in PC12 cells when treated with 1 µM of the I1agonist.5 |
别名 | Oxaminozoline;S 3341; |
供应商 | Cayman |
应用文献 | |
1.Reis, D.J. and Piletz, J.E. The imidazoline receptor in control of blood pressure by clonidine and allied drugs. American Journal of Physiology 273(5 Pt 2), R1569-R1571 (1997). 2.Guyenet, P.G. Is the hypotensive effect of clonidine and related drugs due to imidazoline binding sites? American Journal of Physiology 273(2 Pt 5), R1580-R1584 (1997). 3.Michel, M.C. and Ernsberger, P. Keeping an eye on the I site: Imidazoline-preferring receptors. Trends in Pharamacological Sciences 13(10), 369-370 (1992). 4.Bricca, G.,Dontenwill, M.,Molines, A., et al. Rilmenidine selectivity for imidazoline receptors in human brain. European Journal of Pharmacology 163(2-3), 373-377 (1989). 5.Williams, A.,Sarkar, S.,Cuddon, P., et al. Novel targets for Huntington’s disease in an mTOR-independent autophagy pathway. Nature Chemical Biology 4(5), 295-305 (2008). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 238.3 |
分子式 | C10H16N2O • 1/2C4H4O4 |
CAS号 | 207572-68-7 |
稳定性 | ≥ 2 years |
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