Cirazoline hydrochloride manufacturers
|
| | Cirazoline hydrochloride Basic information |
| Product Name: | Cirazoline hydrochloride | | Synonyms: | 2-[(2-cyclopropylphenoxy)methyl]-4,5-dihydro-1H-imidazolium chloride;CIRAZOLINE HYDROCHLORIDE SELECTIVE A1 AD RENOCE;2-[(2-CYCLOPROPYLPHENOXY)METHYL]-4,5-DIHYDRO-1H-IMIDAZOLE HYDROCHLORIDE;2-(2-CYCLOPROPYLPHENOXYMETHYL)IMIDAZOLINE HYDROCHLORIDE;LD-3098;LD 3098 hydrochloride;Cirazoline hydrochlo;Cirazoline hydrochloride (LD 3098 hydrochloride) | | CAS: | 40600-13-3 | | MF: | C13H17ClN2O | | MW: | 252.74 | | EINECS: | 2549953 | | Product Categories: | Adrenoceptor | | Mol File: | 40600-13-3.mol |  |
| | Cirazoline hydrochloride Chemical Properties |
| storage temp. | Store at RT | | solubility | H2O: >35 mg/mL | | form | solid | | color | white | | Water Solubility | H2O: >35mg/mL | | 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 | | InChIKey | XFRXWLWUUDJHPB-UHFFFAOYSA-N | | SMILES | Cl[H].C1CN=C(COc2ccccc2C3CC3)N1 |
| Safety Statements | 22-24/25 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | Cirazoline hydrochloride Usage And Synthesis |
| Description | Cirazoline is an α1-adrenergic receptor (α1-AR) agonist (Kis = 120, 960, and 660 nM for recombinant α1A-, α1B-, and α1D-ARs, respectively, in CHO cell membranes). It acts as a full agonist at α1A- and a partial agonist at α1B- and α1D-ARs in vitro (EC50s = 70.7, 79.4, and 239.8 nM, respectively). It also acts as an antagonist at α2-ARs with a pA2 value of 7.56 to inhibit the norepinephrine-induced twitch response in isolated pig ileum. Cirazoline (0.01-1 μg/kg) decreases blood pressure when administered via microinjection to the nucleus reticularis lateralis (NRL) of anesthetized normotensive cats. It enhances spatial memory and reduces depressive- and anxiety-like behavior in mice when administered at a concentration of 10 mg/L in drinking water for 2-9 months. It also enhances performance in the variable delayed response task in aged rhesus monkeys at high doses of 1-10 μg/kg but impairs performance at lower doses of 0.01-1 μg/kg. | | Uses | Cirazoline hydrochloride has been used to activate the α1-noradrenergic receptors and to study the inhibitory effect of neurokinin1 (NK1) antagonists on respiratory activity using the brainstem transverse slice. | | Biological Activity | Selective α 1 agonist. Also available as part of the α 1 -Adrenoceptor Tocriset™ and Mixed Adrenergic Tocriset™ . | | Biochem/physiol Actions | Cirazoline is a selective α1-adrenoceptor agonist and also a non-selective ligand for the imidazoline binding site. Cirazoline dereases spatial working memory performance in aged monkeys. | | storage | Store at RT | | References | [1] KUNIKO HONE. Selectivity of the imidazoline α-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned α1-adrenoceptor subtypes[J]. British Journal of Pharmacology, 1995, 116 1: 1611-1618. DOI: 10.1111/j.1476-5381.1995.tb16381.x
[2] ROBERT R. RUFFOLO JR. JAMES E W. RECEPTOR INTERACTIONS OF IMIDAZOLINES: α-ADRENOCEPTORS OF RAT AND RABBIT AORTAE DIFFERENTIATED BY RELATIVE POTENCIES, AFFINITIES AND EFFICACIES OF IMIDAZOLINE AGONISTS[J]. British Journal of Pharmacology, 1982, 77 1: 169-176. DOI: 10.1111/j.1476-5381.1982.tb09283.x
[3] P BOUSQUET J S J Feldman. Central cardiovascular effects of alpha adrenergic drugs: differences between catecholamines and imidazolines.[J]. Journal of Pharmacology and Experimental Therapeutics, 1984, 230 1: 232-236.
[4] VAN A DOZE. Long-term α1A-adrenergic receptor stimulation improves synaptic plasticity, cognitive function, mood, and longevity.[J]. Molecular Pharmacology, 2011, 80 4: 747-758. DOI: 10.1124/mol.111.073734
[5] A.F.T. ARNSTEN J. D J. The Alpha-1 Adrenergic Agonist, Cirazoline, Impairs Spatial Working Memory Performance in Aged Monkeys[J]. Pharmacology Biochemistry and Behavior, 1997, 58 1: Pages 55-59. DOI: 10.1016/s0091-3057(96)00477-7 |
| | Cirazoline hydrochloride Preparation Products And Raw materials |
|