| Identification | Back Directory | [Name]
AcotiaMide | [CAS]
185106-16-5 | [Synonyms]
Acofide
AcotiaMide
ACOTIAMIDUM
185106-16-5
Acotiamide D4
YM443 free base
Z-338 free base
Acotiamide formate salt
N-{2-[bis(1-methylethyl)amino]ethyl}-2-{[(2-hydroxy-4,5-dime...
N-[2-[Bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-4-thiazolecarboxamide
N-(2-(diisopropylamino)ethyl)-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide hydrochloride
4-Thiazolecarboxamide, N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-
N-{2-[bis(1-methylethyl)amino]ethyl}-2-{[(2-hydroxy-4,5-dimethoxyphenyl)carbonyl]amino}-1,3-thiazole-4-carboxamide
Acotiamide D6Q: What is
Acotiamide D6 Q: What is the CAS Number of
Acotiamide D6 Q: What is the storage condition of
Acotiamide D6 Q: What are the applications of
Acotiamide D6 | [Molecular Formula]
C21H30N4O5S | [MDL Number]
MFCD00953661 | [MOL File]
185106-16-5.mol | [Molecular Weight]
450.552 |
| Chemical Properties | Back Directory | [density ]
1.246±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
H2O: 20 mg/mL, clear | [form ]
powder | [pka]
7.38±0.50(Predicted) | [color ]
white to beige | [Water Solubility ]
H2O: 20mg/mL, clear | [InChI]
1S/C21H30N4O5S/c1-12(2)25(13(3)4)8-7-22-20(28)15-11-31-21(23-15)24-19(27)14-9-17(29-5)18(30-6)10-16(14)26/h9-13,26H,7-8H2,1-6H3,(H,22,28)(H,23,24,27) | [InChIKey]
TWHZNAUBXFZMCA-UHFFFAOYSA-N | [SMILES]
CC(C)N(C(C)C)CCNC(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)=O.Cl[H] |
| Hazard Information | Back Directory | [Uses]
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3]. | [Definition]
ChEBI: Acotiamide is a member of salicylamides. | [Biological Activity]
Acotiamide is a potentselective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE). Acotiamide showed no affinity for dopamine D2 or serotonin 5-HT4 receptors but does have activity as a muscarinic antagonist. It acts as a prokinetic drug through acetylcholinesterase inhibition and muscarinic receptor antagonismand has been used for the treatment of functional dyspepsia (FD) involving gastric motility dysfunction. | [in vivo]
Acotiamide (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner[2].
Acotiamide (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with an IC50 value of 1.79 μM[3]. | Animal Model: | Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg)[2] | | Dosage: | 0.3, 1, 3, 10, 30 mg/kg | | Administration: | Intravenous injection; once | | Result: | Increased the postprandial gastric motility. |
| Animal Model: | Male Sprague-Dawley rats (aged 6-7 weeks)[3] | | Dosage: | 0.83 mg/kg | | Administration: | Intravenous injection; once. | | Result: | Effectively improved functional dyspepsia by inhibiting AChE in rat stomach. |
| [References]
[1] Kazuyoshi Y oshii, et al. Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach. Pharmaceutical DOI:10.1007/s11095-015-1787-y
[2] Hiroshi Yamawaki, et al. Acotiamide attenuates central urocortin 2-induced intestinal inflammatory responses, and urocortin 2 treatment reduces TNF-α productions in LPS-stimulated macrophage cell lines. Neurogastroenterol Motil. 2020 Aug;32(8):e13813. DOI:10.1111/nmo.13813
[3] Matsunaga Y, Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride. J Pharmacol Exp Ther. 2011 Mar;336(3):791- DOI:10.1124/jpet.110.174847 |
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