Acotiamide hydrochloride trihydrate - CAS 773092-05-0
Catalog number: 773092-05-0
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H37ClN4O8S
Molecular Weight:
541.06
COA:
Inquire
Targets:
functional dyspepsia;
Description:
Acotiamide, also known as YM-443 and Z-338, is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia.
Purity:
98%
Related CAS:
185104-11-4 (Acotiamide HCl, 1:1); 185106-16-5 (Free base)
Appearance:
Solid powder
Synonyms:
N-(2-(diisopropylamino)ethyl)-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide hydrochloride trihydrate; YM443; YM-443; YM 443; Z338; Z-338; Z 338; Acotiamide; Acotiamide hydrochloride trihydrate; Brand name: Acofide
Solubility:
Soluble in DMSO.
Storage:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years if stored properly
InChIKey:
NPTDXIXCQCFGKC-UHFFFAOYSA-N
InChI:
1S/C21H30N4O5S.ClH.3H2O/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);1H;3*1H2
Canonical SMILES:
O=C(C1=CSC(NC(C2=CC(OC)=C(OC)C=C2O)=O)=N1)NCCN(C(C)C)C(C)C.[H]Cl.[H]O[H].[H]O[H].[H]O[H]
1.Z-338, a newly synthetized carboxyamide derivative, stimulates gastric motility through enhancing the excitatory neurotransmission.
Nakajima T;Nawata H;Ito Y J Smooth Muscle Res. 2000 Apr;36(2):69-81.
We studied the effects of Z-338, a newly synthesized carboxyamide derivative, on autonomic neuroeffector transmission in the guinea-pig stomach in relation to its gastrointestinal prokinetic action, by use of tension recording and microelectrode methods. Z-338 (>10(-8) M) dose-dependently enhanced the amplitude of twitch-like contractions and excitatory junction potentials (EJPs) evoked by single or repetitive electrical field stimulation (EFS) without affecting the non-adrenergic non-cholinergic (NANC) relaxation and inhibitory junction potentials (IJPs) in the circular muscle strips of the guinea-pig stomach. Similar to the action of Z 338, pirenzepine (> 10(-8) M), a muscarinic M1-antagonist, enhanced the EJP amplitude, although AF-DX116 (M2-) and 4-DAMP (M3-antagonists) reduced the EJP amplitude, dose-dependently. The EC50 of the Z-338 and pirenzepine concentration response curves on EJPs were 4.7 x 10(-8) M and 1.0 x 10(-8) M, and Hill coefficients were 0.96 and 0.94 respectively. In addition, Z-338 slightly but significantly enhanced the amplitude of slow waves with or without initial spike. These results provide the first evidence that Z-338 exerts its gastrointestinal prokinetic action mainly through enhancing excitatory neuro effector transmission with no effect on NANC inhibitory neuro-effector transmission in the guinea-pig stomach.
2.[Modulatory mechanisms involved in the parasympathetic excitatory neuro-effector transmission in the airway and gastrointestinal tracts--perspective for a new drug creation].
Ito Y Nihon Yakurigaku Zasshi. 1998 Oct;112 Suppl 1:28P-31P.
It is generally considered that dominant excitatory control of airway and gastrointestinal tract is exerted by the parasympathetic nervous system, and the transmitter output from the nerve terminals, mainly acetylcholine (ACh), is modulated in many ways for example by ACh itself, prostaglandins E series (PGE) neuropeptides and nitric oxide (NO). These modulations are probably due to the suppression of high-voltage-activated calcium channels in the nerve terminals, since, for example, ACh or prostaglandin E1 & E2 selectively suppressed both the N- and R-type Ca2+ currents, through M2 muscarinic and EP3-receptors, respectively in paratracheal ganglion cells. Parasympathetic nervous system also releases nonadrenergic-noncholinergic (NANC) inhibitory neurotransmitters in addition to ACh. The threshold level for ACh and NO release, for example, is almost identical, thereby suggesting the possible interactions between NO and ACh at the post-junctional cites, in addition to the prejunctional inhibitory action of NO to suppress ACh release from the nerve terminal. In this context, NO-donors, including SNAP or Cys-NO, reduced the amplitude of carbachol-induced Ca(2+)-dependent Cl- currents (I infinity h, I alpha(Ca)) dose-dependently (IC50: about 10 microM) in the cat tracheal myocytes, and similar inhibition was also exerted by dibutyryl cGMP (db-cGMP).
3.Prokinetics and fundic relaxants in upper functional GI disorders.
Tack J Curr Opin Pharmacol. 2008 Dec;8(6):690-6. doi: 10.1016/j.coph.2008.09.009. Epub 2008 Oct 27.
Gastrointestinal prokinetics are a heterogeneous class of drugs that stimulate smooth muscle contractions to enhance gastric emptying and intestinal transit. Recently studied prokinetics include antidopaminergic agents (itopride), serotonergic agents (tegaserod and others), and motilin receptor agonists and ghrelin receptor agonists (mitemcinal, TZP101). It has been difficult to establish symptomatic benefit with prokinetic drugs in gastroparesis and functional dyspepsia, because of pathophysiological heterogeneity of the patient populations, a lack of well-accepted endpoints, and inconsistent relationships between changes in motor function and symptomatic outcome. Fundic relaxant drugs are a recent different approach to treatment of gastric motility disorders. Recently studied drugs include drugs under investigation including nitrates, serotonin reuptake blockers, 5-HT(1A) receptor agonists (buspirone and R137696), and muscarinc M1/M2 receptor antagonists (acotiamide or Z-338).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 900510-03-4 PF-3274167

PF-3274167
(CAS: 900510-03-4)

PF-3274167, also known as PF-03274167 or PF-327,4167, is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

CAS 4460-86-0 Asaraldehyde

Asaraldehyde
(CAS: 4460-86-0)

A natural COX-2 inhibitor, exhibiting 17-fold selectivity over COX-1

CAS 5451-09-2 5-Aminolevulinic acid hydrochloride

5-Aminolevulinic acid hydrochloride
(CAS: 5451-09-2)

5-Aminolevulinic acid HCl is an intermediate in heme biosynthesis in the body and the universal precursor of tetrapyrroles. 5-Aminolevulinic acid is used as a p...

CAS 126-17-0 Solasodine

Solasodine
(CAS: 126-17-0)

Solasodine is a neuroprotective antioxidant glycoalkaloid of Solanum species. Solasodine increases superoxide dismutase (SOD), catalase (CAT),and glutathione (G...

CAS 4030-22-2 PYR-0222

PYR-0222
(CAS: 4030-22-2)

A useful intermediate for chemical synthesis

CAS 1263-89-4 Paromomycin Sulfate

Paromomycin Sulfate
(CAS: 1263-89-4)

Paromomycin Sulfate is an aminoglycoside antibiotics inhibiting protein synthesis in non-resistant cells by binding to 16S ribosomal RNA.

CAS 1504588-00-4 NAB 2

NAB 2
(CAS: 1504588-00-4)

NAB 2 can protect against α-synuclein toxicity. It can reverse the α-synuclein-induced pathological phenotype in Parkinson's disease cortical neurons and promot...

CAS 69004-03-1 Toltrazuril

Toltrazuril
(CAS: 69004-03-1)

Toltrazuril is a coccidiostat.

Quick Inquiry

Verification code

Featured Items