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Cirazoline hydrochloride

CAS# 40600-13-3

Cirazoline hydrochloride

2D Structure

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Cirazoline hydrochloride

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Chemical Properties of Cirazoline hydrochloride

Cas No. 40600-13-3 SDF Download SDF
PubChem ID 11957512 Appearance Powder
Formula C13H17ClN2O M.Wt 252.74
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name 2-[(2-cyclopropylphenoxy)methyl]-4,5-dihydro-1H-imidazole;hydrochloride
SMILES C1CC1C2=CC=CC=C2OCC3=NCCN3.Cl
Standard InChIKey XFRXWLWUUDJHPB-UHFFFAOYSA-N
Standard InChI InChI=1S/C13H16N2O.ClH/c1-2-4-12(11(3-1)10-5-6-10)16-9-13-14-7-8-15-13;/h1-4,10H,5-9H2,(H,14,15);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Cirazoline hydrochloride

DescriptionSelective α1 agonist. Also available as part of the α1-Adrenoceptor and Mixed Adrenergic.

Cirazoline hydrochloride Dilution Calculator

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Cirazoline hydrochloride Molarity Calculator

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Preparing Stock Solutions of Cirazoline hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9566 mL 19.7832 mL 39.5664 mL 79.1327 mL 98.9159 mL
5 mM 0.7913 mL 3.9566 mL 7.9133 mL 15.8265 mL 19.7832 mL
10 mM 0.3957 mL 1.9783 mL 3.9566 mL 7.9133 mL 9.8916 mL
50 mM 0.0791 mL 0.3957 mL 0.7913 mL 1.5827 mL 1.9783 mL
100 mM 0.0396 mL 0.1978 mL 0.3957 mL 0.7913 mL 0.9892 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Cirazoline hydrochloride

Binding of [3H]cirazoline to an imidazoline site in rat brain and kidney membranes.[Pubmed:7589165]

Eur J Pharmacol. 1995 May 24;278(3):261-4.

Two classes of high-affinity sites for [3H]cirazoline were characterized in rat brain and kidney membranes. In both tissues, the binding parameters for the high- and low-affinity sites are similar with Bmax values of approximately 50 fmol/mg protein, Kd approximately 0.6 nM and Bmax approximately 470 fmol/mg protein, Kd approximately 11 nM respectively. Inhibition studies of [3H]cirazoline binding to the lower affinity site revealed that only guanidinium or imidazoline derivatives compete with the specific binding of this radioligand. Our results suggest that [3H]cirazoline could be used as a novel ligand to label the non-adrenergic imidazoline-preferring sites.

Further characterization of the guinea pig cerebral cortex idazoxan receptor: solubilization, distinction from the imidazole site, and demonstration of cirazoline as an idazoxan receptor-selective drug.[Pubmed:1972387]

J Neurochem. 1990 Jul;55(1):192-203.

We have demonstrated previously that [3H]idazoxan, besides being able to bind to alpha 2-adrenergic receptors, may also bind to a nonadrenergic idazoxan-receptor site with high affinity. The idazoxan receptor is tightly bound to cellular membranes, and we have now developed a method to solubilize it from the guinea pig cerebral cortex by using the detergent 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS). The CHAPS-solubilized receptor retains its binding properties for drugs: the membrane-bound, as well as the solubilized, idazoxan receptor shows high affinities for a number of imidazolines (cirazoline, idazoxan, tolazoline, naphazoline, tramazoline, clonidine, and oxymetazoline), some imidazoles (medetomidine, detomidine), and guanfacine. By contrast, catecholamines (adrenaline, noradrenaline, isoprenaline, and dopamine) and a number of other neurotransmitters and neuromodulators (serotonin, histamine, glutamic acid, gamma-aminobutyric acid, glycine, and adenosine) show negligible affinities for the idazoxan receptor. Moreover, the idazoxan receptor shows grossly different binding properties for histamine, cimetidine, and imidazole-4-acetic acid compared to what has been described for the nonadrenergic imidazole site labeled by p-[3H]amino-clonidine, indicating that the two receptor sites are distinct. Radioligand binding data further indicate that cirazoline is an idazoxan receptor-selective drug (KD = 1 nM) showing a 50-210-fold selectivity for binding to the idazoxan receptor when compared to alpha 2-adrenergic receptors and an about 500-fold selectivity when compared to alpha 1-adrenergic receptors. We have also reviewed the literature for possible nonadrenergic actions of idazoxan and cirazoline, and we suggest that idazoxan receptors might be involved in the control of prolactin release from the pituitary.

Renal effects of selective alpha-1 and alpha-2 adrenoceptor agonists in conscious, normotensive rats.[Pubmed:2882013]

J Pharmacol Exp Ther. 1987 Mar;240(3):723-8.

The effects of the selective alpha-1 adrenoceptor agonist, cirazoline, and the selective alpha-2 adrenoceptor agonist, B-HT 933, were assessed on renal hemodynamics and on water and solute excretion in conscious, chronically instrumented rats. Infusion (i.v.) of equipressor doses of cirazoline and B-HT 933, 0.04 and 4 mg/kg/hr, respectively, decreased renal plasma flow without changing glomerular filtration rate. Cirazoline infusion did not affect urinary excretion of water, electrolytes or total solutes. In marked contrast, B-HT 933 increased urine flow and sodium excretion significantly (P less than .01) but did not significantly alter potassium and urea excretion. Urine osmolality decreased to hyposmotic levels (from 613 +/- 86 to 172 +/- 8 mOsmol/kg of H2O) during the infusion of B-HT 933, suggesting a possible interaction between the alpha-2 adrenoceptor agonist and the vasopressin system. This diuretic action of the selective alpha-2 adrenoceptor agonist was also observed after the i.v. infusion of a subpressor dose (0.4 mg/kg/hr) of B-HT 933. In rats treated with the ganglionic blocker, hexamethonium (10 mg/kg i.v.), the B-HT 933-induced diuresis was not affected, confirming an action in the periphery, possibly at the level of the kidney. These results suggest that stimulation of renal alpha-2 adrenoceptors in conscious, euvolumic rats modulates the reabsorption of water and sodium at the site of the renal nephron.

Description

Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM).

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