| CAS |
57-37-4 |
| Chinese Name |
盐酸贝那替秦 |
| English Name |
Benactyzine Hydrochloride |
| Synonyms |
Neuroleptone;Tranquilline;Amitakon;胃复康 |
| Molecular Formula |
C20H26ClNO3 |
| Molecular Weight |
363.88 |
| Solubility |
Soluble in Water/DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 200-324-4 |
| MDL |
MFCD00012624 |
| SMILES |
CCN(CC)CCOC(=O)C(C1=CC=CC=C1)(C2=CC=CC=C2)O.Cl |
| InChIKey |
ZCEHOOLYWQBGQO-UHFFFAOYSA-N |
| InChI |
InChI=1S/C20H25NO3.ClH/c1-3-21(4-2)15-16-24-19(22)20(23，17-11-7-5-8-12-17)18-13-9-6-10-14-18;/h5-14，23H，3-4，15-16H2，1-2H3;1H |
| PubChem CID |
66448 |
| Target Point |
Butyrylcholinesterase (BChE) |
| Passage |
Neuronal Signaling |
| Background |
It is a butyryl cholinesterase (BChE) inhibitor. |
| Biological Activity |
Benactyzine Hydrochloride 是一种丁酰胆碱酯酶（BChE）抑制剂，Ki 值为 0.010 mM。[1-2] |
| IC50 |
Ki: 0.010mM(BChE)[1] |
| In Vitro |
After enter the bloodstream，Benactyzine and drofenine will interact with butyrylcholinesterase(BChE; acylcholine acyl hydrolase: EC 3.1.1.8). Both drugs were competitive inhibitors of BChE and the Ki values of benactyzine and drofenine were 0.010 +/- 0.001 and 0.003 +/- 0.000 mM，respectively，drofenine is a more potent competitive inhibitor of BChE than benactyzine.[1] |
| In Vivo |
Benactyzine(1 mg/kg)suppressed the salivation induced by ACH. After pretreatment with imipramine(but not with benactyzine and promazine)5-HT produced vomiting.[2] |
| 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]. |
| 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]. |
| Data Literature Source |
[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.
[2]. Allikmets LH，et alP. Dissimilar influences of imipramine，benactyzine and promazine on effects of micro-injections of noradrenaline，acetylcholine and serotonin into the amygdala in the cat. Psychopharmacologia. 1969;15(5):392-403. |
| Unit |
Bottle |
| Specification |
50mg 100mg |
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