| CAS NO: | 207572-68-7 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 238.3 |
| Cas No. | 207572-68-7 |
| Formula | C10H16N2O·1/2C4H4O4 |
| Synonyms | Oxaminozoline,S 3341 |
| Solubility | ≤10mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide |
| Chemical Name | N-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine, 2E-butenedioate |
| Canonical SMILES | OC(/C=C/C(O)=O)=O.C1(NC(C2CC2)C3CC3)=NCCO1.C4(NC(C5CC5)C6CC6)=NCCO4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Rilmenidine is an 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].
In vitro: Bilateral microinjection of rilmenidine into the C1 area of the rostral ventrolateral medulla (RVL) elicited dose-dependent falls in arterial pressure and heart rate. In RVL, rilmenidine competed with binding to imidazole and α2-adrenergic binding sites with a 30-fold selectivity for the imidazole binding sites [2]. Rilmenidine, a new antihypertensive agent, appeared 2.5 and 3.5 times more selective than clonidine and guanfacine, respectively, for medullary IPR sites than for cortical α-adrenoceptors [3]. Rilmenidine targeted the nonadrenergic imidazoline-binding site I1 receptor with the Ki value of 7.1 nM and demonstrated weaker affinity for the I2 receptor with the Ki value of 5.2 μM [4].
In vivo: In rat model of hypertension associated with insulin resistance, rilmenidine ameliorated the deleterious effects of a high-fructose diet, such as weight gain, hypertension, and resistance to the effects of insulin [5]. In a mouse model of Huntington's disease, rilmenidine induced autophagy, attenuated toxicity of polyglutamine expansions and the signs of disease, reduced the mutant huntingtin fragment levels [6].
References:
[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] Gomez R E, Ernsberger P, Feinland G, et al. Rilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 area[J]. European journal of pharmacology, 1991, 195(2): 181-191.
[3] Bricca G, Dontenwill M, Molines A, et al. Rilmenidine selectivity for imidazoline receptors in human brain[J]. European journal of pharmacology, 1989, 163(2): 373-377.
[4] Guyenet P G. Is the hypotensive effect of clonidine and related drugs due to imidazoline binding sites [J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 1997, 273(5): R1580-R1584.
[5] Penicaud L, Berthault M F, Morin J, et al. Rilmenidine normalizes fructose-induced insulin resistance and hypertension in rats[J]. Journal of hypertension. Supplement: official journal of the International Society of Hypertension, 1998, 16(3): S45-9.
[6] Rose C, Menzies F M, Renna M, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease[J]. Human molecular genetics, 2010, 19(11): 2144-2153.
m.cnreagent.com