PHARMACOLOGICAL STUDIES ON NEW SYNTHETIC ANTITUSSIVE AGENTS

1958 ◽  
Vol 36 (5) ◽  
pp. 475-481 ◽  
Author(s):  
C. I. Chappel ◽  
M.-G. P. Stegen ◽  
G. A. Grant
Keyword(s):  
Clinical Trial ◽  
Chronic Toxicity ◽  
Alkyl Esters ◽  
Antispasmodic Activity ◽  
Pharmacological Studies ◽  
Local Anaesthetic Action ◽  
Antitussive Activity ◽  
Antitussive Agents ◽  
Anaesthetic Action ◽  
Central Depressant

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.

PHARMACOLOGICAL STUDIES ON NEW SYNTHETIC ANTITUSSIVE AGENTS

1958 ◽  
Vol 36 (1) ◽  
pp. 475-481
Author(s):  
C. I. Chappel ◽  
M.-G. P. Stegen ◽  
G. A. Grant
Keyword(s):  
Clinical Trial ◽  
Chronic Toxicity ◽  
Alkyl Esters ◽  
Antispasmodic Activity ◽  
Pharmacological Studies ◽  
Local Anaesthetic Action ◽  
Antitussive Activity ◽  
Antitussive Agents ◽  
Anaesthetic Action ◽  
Central Depressant

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.

Increased sensitivity of frog skeletal muscle to procaine in the presence of organic anions

1978 ◽  
Vol 56 (5) ◽  
pp. 739-746 ◽  
Author(s):  
J. G. Foulks ◽  
F. A. Perry
Keyword(s):  
Action Potentials ◽  
Time Course ◽  
Organic Anion ◽  
Organic Anions ◽  
Depressant Effect ◽  
Alkyl Sulfonates ◽  
Carboxylate Anions ◽  
Increased Sensitivity ◽  
Local Anaesthetic Action ◽  
Anaesthetic Action

In solutions containing an organic anion in place of chloride, frog toe muscles displayed increased sensitivity to the local anaesthetic action of procaine. Twitch inhibition by procaine in all media was accompanied by suppression of action potentials without change in membrane resting potentials. The twitch depressant effect of procaine was greater in solutions with carboxylate anions than with alkyl sulfonates. The intensity and the rapidity of onset of the effects of organic anions was related to the size of their hydrophobic component.Procaine accentuated acetate-induced reductions in the [K]0 required to produce K contractures and in the time course of submaximum K contractures. These effects were not shared by benzocaine. They were antagonized by increased [Ca]0.The results indicate that separate agents can exert mutually enhancing actions from opposite surfaces of the sarcolemma to facilitate the inactivation of depolarization-induced excitation–contraction coupling as well as that of the potential-dependent sodium channel.

scholarly journals Pharmacological Studies on the Chinese Crude Drug"Shoma". III. Central Depressant and Antispasmodic Actions of Cimicifuga Rhizoma, Cimicifuga simplex WORMSK

1980 ◽  
Vol 100 (11) ◽  
pp. 1143-1150 ◽  
Author(s):  
MADOKA SHIBATA ◽  
MIO IKOMA ◽  
MAKOTO ONODA ◽  
FUYUE SATO ◽  
NOBUKO SAKURAI
Keyword(s):  
Crude Drug ◽  
Pharmacological Studies ◽  
Central Depressant

scholarly journals Pharmacological studies on grayanoids. (I). Central depressant action of grayanotoxin (III)

1986 ◽  
Vol 40 ◽  
pp. 192
Author(s):  
Takao Ohgaki ◽  
Kazuo Yanada ◽  
Haruo Meguri ◽  
Yukio Yoneda ◽  
Masao Koida
Keyword(s):  
Depressant Action ◽  
Pharmacological Studies ◽  
Central Depressant

scholarly journals Pethidine has a local anaesthetic action on peripheral nerves in vivo.

Anaesthesia ◽  
1993 ◽  
Vol 48 (5) ◽  
pp. 382-386 ◽  
Author(s):  
P. J. ARMSTRONG ◽  
C. P. J. MORTON ◽  
A. F. NIMMO
Keyword(s):  
Local Anaesthetic ◽  
Peripheral Nerves ◽  
Local Anaesthetic Action ◽  
Anaesthetic Action

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 ◽  
...  
Keyword(s):  
Antitussive Activity ◽  
Antitussive Agents
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