Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , COA of Formula: C8H12N2, 13925-07-0, Name is 2-Ethyl-3,5-dimethylpyrazine, molecular formula is C8H12N2, belongs to piperidines compound. In a document, author is Canale, Vittorio, introduce the new discover.
Synthesis and Pharmacological Evaluation of Novel Silodosin-Based Arylsulfonamide Derivatives as alpha(1A)/alpha(1D)-Adrenergic Receptor Antagonist with Potential Uroselective Profile
Benign prostatic hyperplasia (BPH) is the most common male clinical problem impacting the quality of life of older men. Clinical studies have indicated that the inhibition of alpha(1A)-/alpha(1D) adrenoceptors might offer effective therapy in lower urinary tract symptoms. Herein, a limited series of arylsulfonamide derivatives of (aryloxy)ethyl alicyclic amines was designed, synthesized, and biologically evaluated as potent alpha(1)-adrenoceptor antagonists with uroselective profile. Among them, compound 9 (3-chloro-2-fluoro-N-([1-(2-(2-(2,2,2-trifluoroethoxy)phenoxy]ethyl)piperidin-4-yl) methyl) benzenesulfonamide) behaved as an alpha(1A)-/alpha(1D)-adrenoceptor antagonist (K-i(alpha(1)) = 50 nM, EC50(alpha(1A)) = 0.8 nM, EC50(alpha(1D)) = 1.1 nM), displayed selectivity over alpha(2)-adrenoceptors (K-i(alpha(2)) = 858 nM), and a 5-fold functional preference over the alpha(1B) subtype. Compound 9 showed adequate metabolic stability in rat-liver microsome assay similar to the reference drug tamsulosin (Cl-int = 67 and 41 mu L/min/mg, respectively). Compound 9 did not decrease systolic and diastolic blood pressure in normotensive anesthetized rats in the dose of 2 mg/kg, i.v. These data support development of uroselective agents in the group of arylsulfonamides of alicyclic amines with potential efficacy in the treatment of lower urinary tract symptoms associated to benign prostatic hyperplasia.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem