Sumanirole 马来酸盐

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

[1] http://en.wikipedia.org/wiki/Sumanirole