Details
Stereochemistry | RACEMIC |
Molecular Formula | C16H21NO5S |
Molecular Weight | 339.407 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC(=O)CC(=O)N1CCSC1COC2=C(OC)C=CC=C2
InChI
InChIKey=WSYVIAQNTFPTBI-UHFFFAOYSA-N
InChI=1S/C16H21NO5S/c1-3-21-16(19)10-14(18)17-8-9-23-15(17)11-22-13-7-5-4-6-12(13)20-2/h4-7,15H,3,8-11H2,1-2H3
Moguisteine is a non-narcotic antitussive compound. Moguisteine demonstrated inhibitory effect on rapidly adapting irritant receptors that could account for the antitussigenic effect of this compound. Furthermore, it is possible that ATP-sensitive K(+) channels may be involved in the anti-tussive effect of peripherally acting non-narcotic moguisteine. The drug did not show any toxic effect on the dams and their fetuses, nor did it have any teratogenic effect in either of the tested species. Finally, moguisteine had no adverse effects, either on parturition or on peri-and postnatal survival and/or development of the offspring. It was reported that moguisteine to be effective in reducing cough frequency in chronic cough of bronchitis and COPD. It was recommended for the short-term symptomatic relief of coughing. Preregistration of moguisteine in Italy is discontinued.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7921605
Curator's Comment: poor penetration - 0.01% of the administered dose (guinea-pigs data)
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: Rapidly adapting receptors |
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Target ID: ATP-sensitive potassium channel (guinea pigs) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10794823 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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3570.47 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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1397.87 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
200 mg 3 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11637.72 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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5547.88 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
200 mg 3 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.54 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
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1.57 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30703444 |
200 mg 3 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
MOGUISTEINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg single, oral Highest studied dose Dose: 400 mg Route: oral Route: single Dose: 400 mg Sources: Page: p.169 |
healthy, ADULT n = 4 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 4 Sources: Page: p.169 |
|
200 mg 3 times / day multiple, oral Studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: Page: p.169 |
healthy, ADULT n = 4 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 4 Sources: Page: p.169 |
PubMed
Title | Date | PubMed |
---|---|---|
Clinical trial of the efficacy and safety of moguisteine in patients with cough associated with chronic respiratory diseases. | 1993 |
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Reproductive toxicology of the new antitussive moguisteine. | 1994 Dec |
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Moguisteine: a novel peripheral non-narcotic antitussive drug. | 1994 Jul |
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General toxicology of the new antitussive moguisteine. | 1994 Nov |
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The efficacy and safety of moguisteine in comparison with codeine phosphate in patients with chronic cough. | 1995 Apr |
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Effects of four antitussives on airway neurogenic inflammation in a guinea pig model of chronic cough induced by cigarette smoke exposure. | 2013 Dec |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7613554
100 mg three times a day
Route of Administration:
Oral
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C74536
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ACTIVE MOIETY