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Submit ReviewRilmenidine hemifumarate is an I1-imidazoline binding site selective ligand and α2-adrenoceptor agonist. Possesses greater I1 vs α2 selectivity than the prototypical compound, clonidine. Also thought to enhance autophagy; shown to increase LC3-II levels in PC12 cells.
M. Wt | 238.29 |
Formula | C10H16N2O.½C4H4O4 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 207572-68-7 |
PubChem ID | 45073450 |
InChI Key | LZFATBMLSYHRTC-WXXKFALUSA-N |
Smiles | OC(=O)\C=C\C(O)=O.C1CC1C(NC1=NCCO1)C1CC1.C1CC1C(NC1=NCCO1)C1CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 5.96 | 25 |
The following data is based on the product molecular weight 238.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.25 mM | 16.79 mL | 83.93 mL | 167.86 mL |
1.25 mM | 3.36 mL | 16.79 mL | 33.57 mL |
2.5 mM | 1.68 mL | 8.39 mL | 16.79 mL |
12.5 mM | 0.34 mL | 1.68 mL | 3.36 mL |
References are publications that support the biological activity of the product.
Bricca et al (1994) Human brain imidazoline receptors: Further characterisation with [3H] clon. Eur.J.Pharmacol. 266 25 PMID: 8137880
Bricca et al (1989) Rilmenidine selectivity for imidazoline receptors in human brain. Eur.J.Pharmacol. 163 373 PMID: 2566507
Mammoto et al (1996) Antiarrhythmic action of rilmenidine on adrenaline-induced arrhythmia via central imidazoline receptors in halothane-anaesthetized dogs. Br.J.Pharmacol. 117 1744 PMID: 8732285
Michel and Ernsberger (1992) Keeping an eye on the I site: imidazoline-preferring receptors. TiPS 13 369 PMID: 1413085
Williams et al (2008) Novel targets for Huntington's disease in an mTOR-independent autophagy pathway. Nat.Chem.Biol. 4 295 PMID: 18391949
If you know of a relevant reference for Rilmenidine hemifumarate, please let us know.
Keywords: Rilmenidine hemifumarate, Rilmenidine hemifumarate supplier, α2-adrenoceptor, alpha2-adrenoceptor, a2-adrenoceptor, α2-Adrenergic, alpha2-Adrenergic, a2-adrenergic, agonists, I1, ligand, Receptors, Imidazoline, Adrenergic, Alpha-2, Autophagy, 0790, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Rilmenidine hemifumarate include:
Sánchez-Blázquez et al (2000) Activation of I(2)-imidazoline receptors enhances supraspinal mor. analgesia in mice: a model to detect agonist and antagonist activities at these receptors. Br J Pharmacol 130 146 PMID: 10781010
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