Rilmenidine hemifumarate CAS: 207572-68-7
MF: C10H16N2O•½C4H4O4
MW: 238.29
A selective ligand for I1-imidazoline and α2-AR agonist.

Rilmenidine hemifumarate (CAS 207572-68-7)

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备用名: N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine hemifumarate salt
应用; Rilmenidine hemifumarate is a selective ligand for I1-imidazoline and α2-AR agonist
CAS号码: 207572-68-7
分子量: 238.29
分子式: C10H16N2O•½C4H4O4
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

Rilmenidine hemifumarate is an imidazoline I1 binding site (I1BS)-selective ligand (Ki = 7.1 nM), with much weaker affinity for I2BS (Ki = 5.2 μM). Rilmenidine hemifumarate also acts as an α2-adrenoceptor (α2-AR) agonist. Unlike clonidine (sc-203002), rilmenidine hemifumarate has greater selectivity for I1BS relative to α2-AR.


参考文献

1. Michel, M C., et al., 1992. Keeping an eye on the I site: imidazoline-preferring receptors. Trends in pharmacological sciences. 13(10): 369-70. PMID: 1413085
2. Bricca, G., et al., 1989. Rilmenidine selectivity for imidazoline receptors in human brain. European journal of pharmacology. 163(2-3): 373-7. PMID: 2566507
3. Bricca, G., et al., 1994. Human brain imidazoline receptors: further characterization with [3H]clonidine. European journal of pharmacology. 266(1): 25-33. PMID: 8137880
4. Mammoto, T., et al., 1996. Antiarrhythmic action of rilmenidine on adrenaline-induced arrhythmia via central imidazoline receptors in halothane-anaesthetized dogs. British journal of pharmacology. 117(8): 1744-8. PMID: 8732285

物理状态 :
Solid
溶解度 :
Soluble in DMSO (> 10 mg/ml), ethanol (25 mM), and water (25 mM).
保存 :
Store at -20° C
折射率 :
n20D 1.71 (Predicted)
IC50 :
Plasmodium falciparum W2: IC50 = 12.59 µM; Plasmodium falciparum GB4 : IC50 = 12.59 µM
Ki 数据 :
Nischarin: Ki= 11.22 nM (rat); α2C-AR: Ki= 12.59 nM (human); α2A-AR: Ki= 36.31 nM (human); α2B-AR: Ki= 42.66 nM (human); Nischarin: Ki= 59.2 nM (human)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
RTECS :
RP7207400
PubChem CID :
默克索引 :
14: 8222
MDL 号码 :
MFCD09878261
EC号码 :
259-021-0
SMILES :
OC(=O)/C=C/C(=O)O.C1CN=C(O1)NC(C1CC1)C1CC1.C1CN=C(O1)NC(C1CC1)C1CC1

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