化学名称 : Sumanirole 马来酸盐
CAS : 179386-44-8
英文名称: U-95666E(Sumanirole maleate)/U95666E
英文同义词: SUMANIROLE MALEATE
溶解度:Unknown
储存条件:at -20℃ 2 years
生物活性
Sumanirole maleate is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. It has greater than 200-fold selectivity for the D2 receptor subtype versus the other dopamine receptor subtypes in radioligand binding assays. In cell-based assays, sumanirole is a fully efficacious agonist, with EC50 values between 17 and 75 nM. In animals, sumanirole elicits many physiological responses attributed to D2-like receptor function. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels (ED50 = 12.1 μmol/kg i.p.). Sumanirole s.c. dose dependently decreased plasma prolactin levels and depressed dopamine neuron firing rates in the substantia nigra pars compacta with an ED50 of 2.3 μmol/kg i.v.
参考文献