| Identification | Back Directory | [Name]
RILMENIDINE HEMIFUMARATE SALT | [CAS]
207572-68-7 | [Synonyms]
LZFATBMLSYHRTC-WXXKFALUSA-N
RILMENIDINE HEMIFUMARATE SALT
n-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine hemifumarate salt
Oxaminozoline hemifumarate salt, Rilmenidene hemifumarate salt, N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine hemifumarate salt | [Molecular Formula]
2C10H16N2O.C4H4O4 | [MDL Number]
MFCD00673925 | [MOL File]
207572-68-7.mol | [Molecular Weight]
476.57 |
| Hazard Information | Back Directory | [Uses]
Rilmenidine hemifumarate ┬аis an antihypertensive agent that selectively binds nonadrenergic imidazoline-binding site I1 receptor. | [Biological Activity]
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]. | [Biochem/physiol Actions]
Selective I1 imidazoline receptor agonist. | [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]. | [storage]
Store at -20°C | [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. |
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