1-(4-アミノ-5-クロロ-2-メトキシフェニル)-3-[1-(2-メチルスルホニルアミノエチル)-4-ピペリジニル]-1-プロパノン 化学特性,用途語,生産方法
使用
RS 67506 Hydrochloride is a novel and potent 5-HT4 receptor agonist.
定義
ChEBI: A hydrochloride salt obtained by mixing equimolar amounts of RS 39604 with hydrochloric acid. A potent and selective 5-HT4 antagonist, with a pKi of 9.1 at 5-HT4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A,
2C, 3 and D1, D2, M1, M2, AT1, B1 and alpha1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.
生物活性
A potent and selective 5-HT 4 partial agonist, with a pK i of 8.8 at 5-HT 4 sites in guinea pig striatum, but < 6.0 at several other receptors including 5-HT 1A, 1D, 2A, 2C , D 1 , D 2 and M 1-3 . It is active in vivo and has an intrinsic activity compared to 5-HT of 0.6.
1-(4-アミノ-5-クロロ-2-メトキシフェニル)-3-[1-(2-メチルスルホニルアミノエチル)-4-ピペリジニル]-1-プロパノン 上流と下流の製品情報
原材料
準備製品