Methylscopolamine is an antagonist of muscarinic acetylcholine receptors (Ks = 0.25, 0.37, 0.23, 0.22, and 0.3 nM for M respectively). It inhibits oxotremorine-induced gastric ulcer formation and pupillary light reflex in rats (EDs = 0.4 and 3.6 μg/kg, respectively). It also increases pupil diameter in rats with an ED value of 1.8 μg/kg. Formulations containing methylscopolamine have been used for the treatment of peptic ulcers, intestinal spasms, and motion sickness.
Methylscopolamine (bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice.
体内研究
Methscopolamine (0.25-1.0 mg/kg; subcutaneous injection; Due to the inability to cross the blood-brain barrier, Arecoline cannot counteract the shortening effect of ethanol induced hypnosis duration in mice.
Methscopolamine bromamide (5-10 mg/kg; intraperitoneal injection; Single dose administration can increase the maximum release of acetylcholine in the striatum of freely moving rats by 380% and 430% respectively, without altering their autonomous motor activity.
Animal Model:
ICR mice (male, 18 to 22 g)
Dosage:
0.25 mg/kg; 1.0 mg/kg
Administration:
s.c.; single dose
Result:
Did not significantly alter the duration of ethanol-induced loss of the righting reflex (LORR) compared to saline-treated controls when administered alone.
Did not reverse the arecoline-induced shortening of ethanol-induced LORR duration (no significant difference compared to the saline + arecoline group) when administered before arecoline.
Animal Model:
Wistar rats (male, 280-350 g)
Dosage:
5 mg/kg; 10 mg/kg
Administration:
i.p.; single injection
Result:
Caused a maximal 380% increase in striatal acetylcholine release relative to baseline levels at 2 hours post-injection, with release remaining above baseline for over 4 hours.
Caused a maximal 430% increase in striatal acetylcholine release relative to baseline levels at 2 hours post-injection, with release remaining above baseline for over 4 hours.
Did not cause a change in spontaneous motor activity relative to controls.
分子式
C18H24NO4.Br
分子量
398.29
CAS号
155-41-9
中文名称
甲溴东莨菪碱
运输条件
Room temperature in continental US; may vary elsewhere.