Product Introduction
Bioactivity


英文名: Tolterodine tartrate

描述: Tolterodine tartrate (PNU-200583E) 是毒蕈碱受体的有效拮抗剂。 它在体内显示出对膀胱和唾液腺的选择性。

体外活性: Tolterodine静脉给药增加了正常大鼠和树胶脂毒素治疗大鼠的排尿体积、平均排尿间隔和膀胱容量. 2 nM /kg Tolterodine明显增加对照脑梗死大鼠的膀胱容而不增加残气量,但却对resiniferatoxin-脑梗死大鼠的BC没有影响.Tolterodine酒石酸盐（0.1和1.0 mg/kg）降低膀胱出口梗阻的雌性大鼠的非排尿收缩的数量和振幅,分别达38-74％和29-44％,还增加膀胱容量达19-51％.腹腔注射1 mg/kg Tolterodine给麻醉猫,发现乙酰胆碱诱导的膀胱收缩受到明显抑制,比电致流涎更有效.

体内活性: Tolterodine是一种新型毒蕈碱受体拮抗剂,可用于治疗膀胱过动症及急迫性尿失禁等症状。Tolterodine通过浓度依赖性的方式有效地竞争性抑制豚鼠膀胱隔离条中氨甲酰胆碱诱导的收缩。Tolterodine与毒蕈碱受体亲和力高,在豚鼠膀胱、心脏,、大脑皮层结合、腮腺和人膀胱的Ki 值分别为：2.7 nM、1.6 nM、0.75 nM、4.8 nM、3.3 nM。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 6 mg/mL (12.61 mM)
H2O : 14 mg/mL (29.4 mM)
DMSO : 88 mg/mL (185 mM)


关键字: Tolterodine tartrate | muscarinic | Kabi 2234 | Inhibitor | salivary | mAChR | Tolterodine | urinary | bladder | Tolterodine Tartrate | receptor | inhibit | glands | Kabi2234 | Muscarinic acetylcholine receptor

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相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Anti-Parkinson's Disease Compound Library | ReFRAME Related Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | Bioactive Compound Library