Moguisteine: a novel peripheral non‐narcotic antitussive drug

Gallico, L.; Borghi, A; Rosa, C. Dalla; Ceserani, R.; Tognella, S

doi:10.1111/j.1476-5381.1994.tb13149.x

Cited by 33 publications

(14 citation statements)

References 18 publications

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“…In agreement with published results [12], other cell types, such as macrophages and lymphocytes, did not significantly change in numbers, and are, therefore, not depicted in table 5. With regard to the total cell number, at baseline the value was 6.1×10 6 , at 17 h it was 13.2×10 6 and at 72 h 19.4×10 6 .…”

Section: Late Phase Airway Leucocyte Accumulation In Sensitized Guinesupporting

confidence: 79%

“…Moguisteine, ethyl (R,S)-2-(2-methoxyphenoxy) methyl-β-oxo-3-(1,3-thiazolidine) propanoate, is a novel peripheral nonnarcotic antitussive agent that has proved to be as active as codeine in several experimental models of induced cough in guinea-pigs and dogs [4,5]. It acts neither through the opiate receptors nor on the cough centre, and its action is possibly mediated by the interaction with rapidly adapting irritant receptors along the tracheobronchial tree [4].…”

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confidence: 99%

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Effects of moguisteine, a peripheral nonnarcotic antitussive agent, on airway inflammation in guinea-pigs in vivo

Gallico¹,

Oggioni²,

Rosa³

et al. 1996

Eur Respir J

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Cough is a common symptom of respiratory diseases associated with irritation or inflammation of the airways, and symptomatic antitussive drugs are frequently prescribed to control an abnormal cough reflex. Our aim was to evaluate the effects of moguisteine, a novel, peripheral, nonnarcotic antitussive agent, on airway inflammation induced in guinea-pigs with a variety of stimuli.These stimuli included exposure to tobacco smoke for 10 min, to elicit airway hyperreactivity, eosinophil recruitment in bronchoalveolar lavage (BAL), airway epithelial damage and plasma exudation; graded platelet-activating factor (PAF) infusion (600 ng·kg -1 over one h), to induce airway hyperreactivity; 2% ovalbumin (OA) aerosol challenge in 1% OA-sensitized animals, to induce late-phase (17 and 72 h) airway leucocyte accumulation. We also assessed the activity of moguisteine on plasma leakage induced by capsaicin, on bronchoconstriction induced by acetylcholine (ACh), histamine (H) and PAF, and on leukotriene mediated allergic bronchospasm in OA-sensitized guinea-pig.Moguisteine (p.o. and i.m.) and dexamethasone (p.o. and i.m.) dose-dependently reduced tobacco smoke-induced bronchial hyperreactivity. Moguisteine and dexamethasone abolished eosinophil recruitment in BAL, prevented the sloughing of the epithelium and significantly reduced airway microvascular leakage. Both agents were also highly effective in reducing bronchial hyperreactivity elicited by PAF infusion. In addition, moguisteine was active in inhibiting airway neutrophil and eosinophil accumulation in BAL observed 17 and 72 h after OA challenge in sensitized guinea-pigs. In contrast to dexamethasone, moguisteine did not prevent capsaicin-induced plasma leakage. It was also ineffective against bronchoconstriction as induced by ACh, H, and PAF and failed to inhibit leukotriene-dependent bronchospasm.Our data suggest that moguisteine represents an antitussive compound endowed with interesting airway anti-inflammatory properties in guinea-pigs in vivo. Its mechanism of action remains to be elucidated.

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Section: Late Phase Airway Leucocyte Accumulation In Sensitized Guinesupporting

confidence: 79%

mentioning

confidence: 99%

Effects of moguisteine, a peripheral nonnarcotic antitussive agent, on airway inflammation in guinea-pigs in vivo

Gallico¹,

Oggioni²,

Rosa³

et al. 1996

Eur Respir J

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“…In guinea-pigs, moguisteine was found to reduce cough elicited by citric acid inhalation and electrical stimulation of the airway mucosa as effectively as codeine and dextromethorphan [2]. Moguisteine, injected into the cerebral ventricles of guinea-pigs, does not inhibit electrically stimulated cough, which is, instead, effectively blocked by intraventricular codeine: these findings suggest that the antitussive action of moguisteine depends on a peripheral mechanism [3]. Naloxone, a known narcotic antagonist, reverses the antitussive effects of codeine, but not those of moguisteine, indicating that the effects of moguisteine do not involve any interaction with opiate receptors.…”

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confidence: 71%

Action of moguisteine on the activity of tracheobronchial rapidly adapting receptors in the dog

Sant’Ambrogio¹,

Sant'Ambrogio²

1998

Eur Respir J

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Moguisteine is an antitussive agent with a novel chemical structure [1]. Its pharmacological activity has been tested on experimental animals and in several clinical trials. In guinea-pigs, moguisteine was found to reduce cough elicited by citric acid inhalation and electrical stimulation of the airway mucosa as effectively as codeine and dextromethorphan [2]. Moguisteine, injected into the cerebral ventricles of guinea-pigs, does not inhibit electrically stimulated cough, which is, instead, effectively blocked by intraventricular codeine: these findings suggest that the antitussive action of moguisteine depends on a peripheral mechanism [3]. Naloxone, a known narcotic antagonist, reverses the antitussive effects of codeine, but not those of moguisteine, indicating that the effects of moguisteine do not involve any interaction with opiate receptors. The antitussive action of moguisteine is also accompanied by clear anti-inflammatory effects in conditions characterized by bronchial hyperreactivity, airway leucocyte recruitment and airway microvascular leakage [4,5]. These anti-inflammatory effects of moguisteine have been found to be as strong as those of dexamethasone [4,5]. Several clinical trials have substantiated the beneficial effects of moguisteine on coughs of various nature: upper airway infection, chronic bronchitis, pulmonary fibrosis and tumours [6][7][8][9][10][11].Since cough is a reflex response elicited through the activation of specialized receptors activated by exogenous irritants and/or spontaneously occurring pathological conditions, the antitussive action of moguisteine could be viewed as dependent on an inhibitory effect on rapidly adapting irritant receptors (RARs). Indeed, the aim of this study was to investigate the possible effect of moguisteine on the activity of tracheobronchial RARs.RARs, as first identified by KELLER and LOESER [12] and later characterized with single fibre recordings by KNOWLTON and LARRABEE [13], represent a group of airway stretch receptors that respond to maintained lung in-flation and deflation with a rapidly adapting discharge at a highly irregular pattern of discharge. The rate of adaptation varies considerably among RARs, with the most rapidly adapting endings responding only during changes in stretch with a behaviour similar to Pacinian corpuscles, showing a clear off-response at the removal of the stim-ulus [14]. RARs are very responsive to intraluminal stim-uli, mechanical probing of the mucosa, inhalation of inert dust, inflammatory mediators and oedema of the airway walls [15]; for this reason they have also been called irritant receptors [16]. The mechanosensitivity (response to inflation) of RARs is second only to that of slowly adapting receptors and higher than that of pulmonary and bronchial C-fibre endings [17].RARs of similar nature are located superficially within the mucosa of both larynx and tracheobronchial tree [18]. RARs located in the large extrapulmonary tracheobronchial airways (trachea, main stem bronchi and proximal When the results a...

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“…Morphine and naloxone were subcutaneously injected 30 and 15 min, respectively, before the capsaicin challenge. We employed LY303870 at the dose sufficient to block the NK1 receptor-mediated response (4), chlorpheniramine and clemastine at doses sufficient to antagonize histamine H1 receptor (5), and codeine at 20 mg /kg, a dose reported to inhibit the cough response in guinea pigs (6). Data are shown as means ± S.E.M.…”

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confidence: 99%

Inhibitory Effect of Olopatadine Hydrochloride on the Sneezing Response Induced by Intranasal Capsaicin Challenge in Guinea Pigs

Kaise

Akamatsu

Ohmori

et al. 2001

Japanese Journal of Pharmacology

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ABSTRACT-To investigate the possible inhibitory effect of olopatadine hydrochloride (olopatadine), an antiallergic drug, on the tachykinin-mediated nasal responses, we examined the effect of olopatadine on the sneezing and the nasal rubbing responses induced by intranasal capsaicin challenge in guinea pigs. Olopatadine (10 mg/kg, p.o.) inhibited the sneezing response by 57% without affecting the nasal rubbing one. The antihistamines chlorpheniramine and clemastine did not affect the responses. Morphine caused the inhibition of both responses, which was antagonized by naloxone. These results suggest that olopatadine inhibits the sneezing response by the inhibition of the tachykinin release and not by its antihistaminic action.

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Moguisteine: a novel peripheral non‐narcotic antitussive drug

Cited by 33 publications

References 18 publications

Effects of moguisteine, a peripheral nonnarcotic antitussive agent, on airway inflammation in guinea-pigs in vivo

Effects of moguisteine, a peripheral nonnarcotic antitussive agent, on airway inflammation in guinea-pigs in vivo

Action of moguisteine on the activity of tracheobronchial rapidly adapting receptors in the dog

Inhibitory Effect of Olopatadine Hydrochloride on the Sneezing Response Induced by Intranasal Capsaicin Challenge in Guinea Pigs

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