| 摘要 |
<p>A formulation comprises phenoxyacetic acid derivative or its salt. A formulation comprises phenoxyacetic acid derivative of formula (I) or its salt. [Image] X and Y : chiral carbon atom; R 1OH,1-6C alkoxy, aryl-1-6C alkoxy, primary amino or mono-/di-(1-6C alkyl)amino; R 2and R 3H, halo, 1-6C alkyl, trifluoromethyl or 1-6C alkoxy; and R 4H, 1-6C alkyl, halo(1-6C alkyl), hydroxy, 1-6C alkoxy, aryl-1-6C alkoxy, 1-6C alkoxy, cyano, nitro, amino, mono- or di(1-6C alkyl)amino, carbamoyl, mono- or di(1-6C alkyl)carbamoyl or NHCOR 5; R 5H or 1-6C alkyl. Provided that at least one of R 2and R 3is H. ACTIVITY : None given. MECHANISM OF ACTION : Adrenoreceptor-beta -3 agonist. Effect of (-)-2-[4-(2-{(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino}ethyl)-2,5-dimethylphenoxyl] acetic acid (A1) on the tone of monkey detrusor was studied. The detrusor of cynomolgus monkey was isolated and dissected. Tracheal, atrial and urethral dissections were also prepared. The results were as follows: EC 50value of (A1)/isoproterenol was 8.2X10 ->7>. (A1) Exhibited lesser effect on the trachea and atria. The detrusor selectivity of (A1) was 1200 times greater (compared with the trachea) and 80 times greater (compared with the atria). (A1) Showed no effect on endothelin-1-induced tonic contraction of the isolated urethra.</p> |
