113418-56-7
中文名稱
113418-56-7
英文名稱
3,7-Dihydro-1,3-dimethyl-7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-1H-purine-2,6-dione
CAS
113418-56-7
分子式
C28H33N5O3
分子量
487.59
MOL 文件
113418-56-7.mol
更新日期
2023/03/17 20:03:06
113418-56-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T13352化合物WY 49051
英文別名
Wy-490513,7-Dihydro-1,3-dimethyl-7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-1H-purine-2,6-dione
1H-Purine-2,6-dione, 7-[3-[4-(diphenylmethoxy)-1-piperidinyl]propyl]-3,7-dihydro-1,3-dimethyl-
物理化學(xué)性質(zhì)
沸點(diǎn)672.7±65.0 °C(Predicted)
密度1.25±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)8.32±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
Wy 49051 是一種有效的，可口服的 H1 receptor 拮抗劑，IC50 值為 44 nM。靶點(diǎn)
IC50: 44 nM (H1 receptor)
體外研究
Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC 50 of 8 nM.
體內(nèi)研究
Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with ED 50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv. The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment.