LG 30435 is a new bronchodilator agent with multiple sites of action. 1986

A Subissi, and M Criscuoli, and A R Renzetti

LG 30435, a new quaternary derivative of the H1-histamine antagonist mequitazine, was evaluated against bronchospasm induced by different agonists. This compound inhibited equipotently methacholine- and histamine-induced contractions of isolated guinea-pig trachea. When administered to guinea-pig by the i.v. and/or the aerosol route, LG 30435 inhibited dose dependently the bronchospasm induced by acetylcholine and histamine and to a lesser degree that induced by 5-hydroxytryptamine and LTD4. When compared to that of mequitazine, its potency was higher in each case, up to 500-fold when tested in vitro against methacholine. LG 30435 also counteracted antigen-induced bronchospasm both in passively sensitized guinea-pigs and in actively sensitized rats. This compound had a rapid onset of action and an adequate duration after aerosol administration. It was poorly absorbed both by the oral and the aerosol routes and it did not appear to penetrate the blood-brain barrier. These results show that LG 30435 is a new aerosol bronchodilator agent, which, due to its multiple pharmacodynamic actions and to its suitable pharmacokinetics, is potentially useful in the therapy of obstructive airways disease.

UI MeSH Term Description Entries
D008297 Male Males
D010095 Oxotremorine A non-hydrolyzed muscarinic agonist used as a research tool. Oxytremorine
D010640 Phenothiazines Compounds containing dibenzo-1,4-thiazine. Some of them are neuroactive.
D001993 Bronchodilator Agents Agents that cause an increase in the expansion of a bronchus or bronchial tubes. Bronchial-Dilating Agents,Bronchodilator,Bronchodilator Agent,Broncholytic Agent,Bronchodilator Effect,Bronchodilator Effects,Bronchodilators,Broncholytic Agents,Broncholytic Effect,Broncholytic Effects,Agent, Bronchodilator,Agent, Broncholytic,Agents, Bronchial-Dilating,Agents, Bronchodilator,Agents, Broncholytic,Bronchial Dilating Agents,Effect, Bronchodilator,Effect, Broncholytic,Effects, Bronchodilator,Effects, Broncholytic
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006633 Histamine Antagonists Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only. Antihistamine,Antihistamines,Histamine Antagonist,Antagonist, Histamine,Antagonists, Histamine
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D000109 Acetylcholine A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. 2-(Acetyloxy)-N,N,N-trimethylethanaminium,Acetilcolina Cusi,Acetylcholine Bromide,Acetylcholine Chloride,Acetylcholine Fluoride,Acetylcholine Hydroxide,Acetylcholine Iodide,Acetylcholine L-Tartrate,Acetylcholine Perchlorate,Acetylcholine Picrate,Acetylcholine Picrate (1:1),Acetylcholine Sulfate (1:1),Bromoacetylcholine,Chloroacetylcholine,Miochol,Acetylcholine L Tartrate,Bromide, Acetylcholine,Cusi, Acetilcolina,Fluoride, Acetylcholine,Hydroxide, Acetylcholine,Iodide, Acetylcholine,L-Tartrate, Acetylcholine,Perchlorate, Acetylcholine
D000336 Aerosols Colloids with a gaseous dispersing phase and either liquid (fog) or solid (smoke) dispersed phase; used in fumigation or in inhalation therapy; may contain propellant agents. Aerosol
D000707 Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death. Anaphylactic Reaction,Anaphylactoid Reaction,Anaphylactoid Shock,Shock, Anaphylactic,Anaphylactic Reactions,Anaphylactic Shock,Anaphylactoid Reactions,Reaction, Anaphylactic,Reaction, Anaphylactoid,Shock, Anaphylactoid

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