| Description | Fluparoxan is a potent α2-adrenergic receptor antagonist (pKB = 7.9) with excellent α2/α1 selectivity (2630 fold). |
| Synonyms | GR50360, GR 50360, Fluparoxan hydrochloride, GR-50360A, GR-50360 |
| molecular weight | 231.65 |
| Molecular formula | C10H11ClFNO2 |
| CAS | 105226-30-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Borthwick AD. Fluparoxan: A Comprehensive Review of its Discovery, Adrenergic and CNS activity and treatment of Cognitive Dysfunction in central Neurodegenerative diseases. Mini Rev Med Chem. 2016 Mar 21. [Epub ahead of print] PubMed PMID: 26996616. 2. Chu X, Ågmo A. The adrenergic α2-receptor, sexual incentive motivation and copulatory behavior in the male rat. Pharmacol Biochem Behav. 2016 May;144:33-44. doi: 10.1016/j.pbb.2016.02.008. Epub 2016 Feb 22. PubMed PMID: 26906229. 3. Scullion GA, Kendall DA, Marsden CA, Sunter D, Pardon MC. Chronic treatment with the α2-adrenoceptor antagonist fluparoxan prevents age-related deficits in spatial working memory in APP×PS1 transgenic mice without altering β-amyloid plaque load or astrocytosis. Neuropharmacology. 2011 Feb-Mar;60(2-3):223-34. doi: 10.1016/j.neuropharm.2010.09.002. Epub 2010 Sep 17. PubMed PMID: 20850464. 4. Pauwels PJ, Tardif S, Wurch T, Colpaert FC. Facilitation of constitutive alpha(2A)-adrenoceptor activity by both single amino acid mutation (Thr(373)Lys) and g(alphao) protein coexpression: evidence for inverse agonism. J Pharmacol Exp Ther. 2000 Feb;292(2):654-63. PubMed PMID: 10640303. |