Benactyzine hydrochloride
(Synonyms: 胃复康) 目录号 : GC31193Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
Cas No.:57-37-4
Sample solution is provided at 25 µL, 10mM.
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Kinase experiment: | Butyrylcholinesterase activity is measured spectrophotometrically with spectrophotometer using butyrylthiocholine iodide (BTCh) as substrate. In the kinetic studies, initial velocities are measured at 37°C by using 0.25 mM 5,5’-dithio-bis(2-nitrobenzoic acid) (DTNB) in 5 mM 3-(N-morpholino)propanesulfonic acid (MOPS) buffer, pH 7.5, and appropriate concentrations of Benactyzine hydrochloride and drofenine solutions prepared in water, as a function of BTCh concentration from 0.25 to 5.0 mM BTCh in 0.5 mL final volume of assay mixture (0.5 mL assay mixture contains 1.56 mg purified enzyme). Assays are carried out in duplicate and activities are measured for up to 90 s[1]. |
Animal experiment: | Experiments are carried out in 36 cats of both sexes weighing 1.8 to 4 kg in a free-behavior situation. The experiments are carried out in the following order: after the first micro-injection of acetylcholine and/or serotonin and/or noradrenaline (200 μg) into the amygdala the changes in the behavior, autonomic reactions and EEG are recorded for a period of 10 min and then followed by intramuscular injections of imipramine and/or Benactyzine hydrochloride and/or promazine and/or saline (in control experiments). The second micro-injection of neurohormones (200 μg) into the amygdala is performed in 45 rain after the intramuscular injection of drugs and/or saline, and the effect is compared with the previous one, induced by the first micro-injection[2]. |
References: [1]. Bodur E, et al. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch Biochem Biophys. 2001 Feb 1;386(1):25-9. |
Benactyzine hydrochloride is a centrally acting muscarinic antagonist. It is used as an antidepressant in the treatment of depression and associated anxiety.
[1] Amitai G, et al. Mol Pharmacol. 1987, 32(5):678-85. [2] Hana Svobodova, et al. Mil Med Sci Lett (Voj Zdrav Listy). 2011, 80(4): 142-149.
Cas No. | 57-37-4 | SDF | |
别名 | 胃复康 | ||
Canonical SMILES | O=C(OCCN(CC)CC)C(C1=CC=CC=C1)(O)C2=CC=CC=C2.[H]Cl | ||
分子式 | C20H26ClNO3 | 分子量 | 363.88 |
溶解度 | DMSO : 150 mg/mL (412.22 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.7482 mL | 13.7408 mL | 27.4816 mL |
5 mM | 0.5496 mL | 2.7482 mL | 5.4963 mL |
10 mM | 0.2748 mL | 1.3741 mL | 2.7482 mL |
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Effects of benactyzine hydrochloride on dynamic vision functions
We have investigated the effects of an anticholinergic drug, benactyzine HCl on vision and vision function. Our experiments assess the time course and severity of benactyzine effects on visual acuity for static and moving targets, amplitude and dynamics of accommodation, pupil response to light and the spatial contrast sensitivity function. A single dose of the drug (4.14 mg/70 kg body weight, which is within the therapeutic range) and placebo were administered intramuscularly to 12 subjects. Large and significant decrements in visual function were demonstrated after the administration of benactyzine, particularly for those functions performed at near focus. The drug effect was rapid in onset, beginning 7-10 min after injection, peaked at approximately 30-40 min, and declined to baseline values over the next 2 h. The drug increased pulse rate and blood pressure, and induced an intoxicated state involving loss of concentration, attention, and short-term memory.