Structure−Antitussive Activity Relationships of Naltrindole Derivatives. Identification of Novel and Potent Antitussive Agents

2008 ◽  
Vol 51 (15) ◽  
pp. 4404-4411 ◽  
Author(s):  
Satoshi Sakami ◽  
Masayuki Maeda ◽  
Koji Kawai ◽  
Takumi Aoki ◽  
Kuniaki Kawamura ◽  
...  
1958 ◽  
Vol 36 (1) ◽  
pp. 475-481
Author(s):  
C. I. Chappel ◽  
M.-G. P. Stegen ◽  
G. A. Grant

In an attempt to overcome the inherent disadvantage of narcotic antitussive therapy, three basic alkoxy-alkyl esters of phenothiazine-10-carboxylic acid were synthesized and tested for pharmacological activity. These compounds possessed antitussive activity in the cat in the range of activity of codeine. Dimethyl-amino-ethoxy-ethyl phenothiazine-10-carboxylate was chosen, on the basis of strong antitussive activity coupled with low acute toxicity and low antispasmodic activity, for chronic toxicity studies and clinical trial. This compound is devoid of central depressant or analgesic properties and possesses a moderate local anaesthetic action.


1958 ◽  
Vol 36 (5) ◽  
pp. 475-481 ◽  
Author(s):  
C. I. Chappel ◽  
M.-G. P. Stegen ◽  
G. A. Grant

In an attempt to overcome the inherent disadvantage of narcotic antitussive therapy, three basic alkoxy-alkyl esters of phenothiazine-10-carboxylic acid were synthesized and tested for pharmacological activity. These compounds possessed antitussive activity in the cat in the range of activity of codeine. Dimethyl-amino-ethoxy-ethyl phenothiazine-10-carboxylate was chosen, on the basis of strong antitussive activity coupled with low acute toxicity and low antispasmodic activity, for chronic toxicity studies and clinical trial. This compound is devoid of central depressant or analgesic properties and possesses a moderate local anaesthetic action.


2020 ◽  
Author(s):  
HeeKyung Choi ◽  
Won Suk Choi ◽  
Euna Han

BACKGROUND Influenza is an important public health concern. A national surveillance system that easily and rapidly detects influenza epidemics is lacking. OBJECTIVE We assumed that the rate of influenza-like illness (ILI) related-claims is similar to the current ILI surveillance system. METHODS We used the Health Insurance Review and Assessment Service-National Patient Samples (HIRA-NPS), 2014-2018. We defined ILI-related claims as outpatient claims that contain both antipyretic and antitussive agents and calculated the weekly rate of ILI-related claims. We compared ILI-related claims and weekly ILI rates from clinical sentinel surveillance data. RESULTS We observed a strong correlation between the two surveillance systems each season. The absolute thresholds for the four-years were 84.64 and 86.19 cases claims per 1,000 claims for claims data and 12.27 and 16.82 per 1,000 patients for sentinel data (Figure 5). Both the claims and sentinel data surpassed the epidemic thresholds each season. The peak epidemic in the claims data was reached one to two weeks later than in the sentinel data. The epidemic patterns were more similar in the 2016-2017 and 2017-2018 seasons than the 2014-2015 and 2015-2016 seasons. CONCLUSIONS Based on hospital reports, ILI-related claims rates were similar to the ILI surveillance system. ILI claims data can be loaded to a drug utilization review system in Korea to make an influenza surveillance system.


Tetrahedron ◽  
2008 ◽  
Vol 64 (44) ◽  
pp. 10155-10161 ◽  
Author(s):  
Li-Gen Lin ◽  
Henry Pak-Ho Leung ◽  
Jian-Yu Zhu ◽  
Chun-Ping Tang ◽  
Chang-Qiang Ke ◽  
...  

1984 ◽  
Vol 17 (5) ◽  
pp. 521-524 ◽  
Author(s):  
KH Ruhle ◽  
D Criscuolo ◽  
HA Dieterich ◽  
D Kohler ◽  
G Riedel

1998 ◽  
Vol 36 (2) ◽  
pp. 140-143 ◽  
Author(s):  
T. Bhakta ◽  
Pulok K. Mukherjee ◽  
Kakali Saha ◽  
M. Pal ◽  
B.P. Saha

2010 ◽  
Vol 109 (4) ◽  
pp. 1002-1010 ◽  
Author(s):  
Donatella Mutolo ◽  
Fulvia Bongianni ◽  
Elenia Cinelli ◽  
Tito Pantaleo

We have previously shown that the caudal nucleus tractus solitarii is a site of action of some antitussive drugs and that the caudal ventral respiratory group (cVRG) region has a crucial role in determining both the expiratory and inspiratory components of the cough motor pattern. These findings led us to suggest that the cVRG region, and possibly other neural substrates involved in cough regulation, may be sites of action of antitussive drugs. To address this issue, we investigated changes in baseline respiratory activity and cough responses to tracheobronchial mechanical stimulation following microinjections (30–50 nl) of some antitussive drugs into the cVRG of pentobarbital-anesthetized, spontaneously breathing rabbits. [d-Ala2, N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO) and baclofen at the lower concentrations (0.5 mM and 0.1 mM, respectively) decreased cough number, peak abdominal activity, and peak tracheal pressure and increased cough-related total cycle duration (Tt). At the higher concentrations (5 mM and 1 mM, respectively), both drugs abolished the cough reflex. DAMGO and baclofen also affected baseline respiratory activity. Both drugs reduced peak abdominal activity, while only DAMGO increased Tt, owing to increases in expiratory time. The neurokinin-1 (NK1) receptor antagonist CP-99,994 (10 mM) decreased cough number, peak abdominal activity, and peak tracheal pressure, without affecting baseline respiration. The NK2 receptor antagonist MEN 10376 (5 mM) had no effect. The results indicate that the cVRG is a site of action of some antitussive agents and support the hypothesis that several neural substrates involved in cough regulation may share this characteristic.


Author(s):  
SHIKHA SANORIA ◽  
ZULFKAR LATIEF QADRIE ◽  
SURYA PRAKASH GAUTAM ◽  
AMIT BARWAL

Cassia fistula Linn. is also called a “golden shower”. It is aboriginal to India, Sri Lanka and diffused in various countries, including Mexico, China, Mauritius, East Africa, South Africa, and West Indies. Plant and its parts, such as bark, fruit, leaves, and seeds, are used traditionally to cure diseases. Traditionally the plant possesses hepatoprotective, antipyretic, anti-inflammatory, leukotriene inhibition, antitussive activity, antioxidant, wound healing, hypo-lipidemia, anticancer, antidiabetic, central nervous system activity, antiulcer, antibacterial, antifertility, larvicidal and ovicidal, antifeedant, laxative, anti-epileptic, antimicrobial, urease inhibition, antifungal, anti-tobacco mosaic virus activities. The review contains botanical information, constituents and pharmacological leverages of the plant. The review draws attention towards the traditional, phytochemical and pharmacological knowledge accessible on Cassia fistula Linn, which would be beneficial for research scholars to develop novel chemical entities. This review article is written after studying most of the journal’s articles, which were published between 1998 to 2019.


1954 ◽  
Vol 7 (2) ◽  
pp. 119-139 ◽  
Author(s):  
Joachim S. Gravenstein ◽  
Robert A. Devloo ◽  
Henry K. Beecher
Keyword(s):  

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