Oxybutynin hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Oxybutynin chloride 是一种口服有效的、竞争性的 mAChR 拮抗剂，其在小鼠膀胱和大脑皮层中特异性 [3H]NMS 结合的 Ki 值分别为 14.3 和 5.55 nM。Oxybutynin chloride 能够以不依赖其抗胆碱能效应的方式抑制血管 Kv 通道，IC50 值为 11.51 μM。Oxybutynin chloride 能有效减少膀胱和尿路的肌肉痉挛，可用于膀胱过度活动症的研究。

Oxybutynin is also a possible treatment of hyperhidrosis (hyper-active sweating) .(In Vitro):Oxybutynin chloride (0.1, 0.3, 1, 3, 10, 30, 100 μM; 200 ms) inhibits vascular Kv channels in a concentration-dependent manner independent of anticholinergic effect in coronary arterial smooth muscle cells. (In Vivo):Oxybutynin chloride (27.2 mg/kg; p.o.; single) exhibits significant binding of mouse brain muscarinic receptors that about a 2-fold increase in Kd values for specific [3H]N-methylscopolamine binding 0.5 and 2 h later.

Oxybutynin chloride (0.1, 0.3, 1, 3, 10, 30, 100 μM; 200 ms) inhibits vascular Kv channels in a concentration-dependent manner independent of anticholinergic effect in coronary arterial smooth muscle cells. Cell Viability Assay Cell Line:Coronary arterial smooth muscle cells (from Male New Zealand White rabbits)Concentration:10 μM Incubation Time:200 ms Result:Rapidly inhibited the Kv current within 2 min and reduced the Kv current by 44% at +60 Mv.Inhibited the Kv current by changing the gating properties of Kv channels.Cell Viability Assay Cell Line: Coronary arterial smooth muscle cells (from male New Zealand White rabbits)Concentration:0.1, 0.3, 1, 3, 10, 30, 100 μM Incubation Time:200 ms Result:Reduced the Kv current amplitude in a concentration-dependent manner, with an IC50 value of 11.51 μM.

Oxybutynin chloride (27.2 mg/kg; p.o.; single) exhibits significant binding of mouse brain muscarinic receptors that about a 2-fold increase in Kd values for specific [3H]N-methylscopolamine binding 0.5 and 2 h later. Animal Model:Male ddY strain mice (9 to 13-week-old).Dosage:27.2 mg/kg (76.1 μmol/kg) Administration:Oral administration; single.Result:Significant increased Kd values for specific [3H]NMS binding in mouse bladder with values of 54.7% and 40.6% when at 0.5 and 2 hours, respectively. Significant increased Kd values for specific [3H]NMS binding in mouse cerebral cortex with values of 120% and 71.2% when at 0.5 and 2 hours, respectively.

MJ4309-1

Endocrinology/Hormones

AChR

mAChR

Neurological Disease

——

1508-65-2

393.96

C22H32ClNO3

>98% (HPLC)

Ethanol: 79 mg/mL (200.53 mM); Water: 4 mg/mL (10.15 mM); DMSO: 79 mg/mL (200.53 mM)

O=C(OCC#CCN(CC)CC)C(O)(C1CCCCC1)C2=CC=CC=C2.[H]Cl

4-Diethylaminobut-2-ynyl 2-cyclohexyl-2-hydroxy-2-phenylethanoate Hydrochloride

(-20℃)

With Ice Pack

≥ 2 years