Bronchospasmolytic effects of RU 42173.
The bronchodilator properties of RU 42173, a new beta-adrenergic stimulant with an original structure, as a cyclic analogue of an arylethanolamine, have been evaluated on different in vitro and in vivo models and compared with those of salbutamol and isoprenaline. RU 42173 equipotently inhibited histamine-, acetylcholine-, and KCl-induced contractions in isolated guinea pig trachea or small bronchus and in isolated human bronchus. When administered to guinea pigs by the IV or aerosol route, RU 42173 dose-dependently inhibited bronchospasm induced by histamine, acetylcholine, and methacholine. It also inhibited PAF-induced bronchoconstriction and PAF-induced hyperreactivity to histamine. Moreover, RU 42173 had a rapid onset and prolonged duration of action. The potency of RU 42173 was similar to that of salbutamol.
Fichelle
J
J
Centre de Recherches Roussel Uclaf, Romainville, France.
Naline
E
E
Freslon
J L
JL
Jouquey
S
S
Plassard
G
G
Thompson
M A
MA
Miller
P
P
Advenier
C
C
D000109:Acetylcholine / Q000494:pharmacology; D000420:Albuterol / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D001562:Benzimidazoles / Q000494:pharmacology*; D001980:Bronchi / Q000187:drug effects; D001986:Bronchial Spasm / Q000139:chemically induced / Q000188:drug therapy*; D001993:Bronchodilator Agents / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D008688:Methacholine Compounds / Q000494:pharmacology; D010972:Platelet Activating Factor / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects
D001562:Benzimidazoles; D001993:Bronchodilator Agents; D008688:Methacholine Compounds; D010972:Platelet Activating Factor; D006632:Histamine; D007545:Isoproterenol; D000109:Acetylcholine; D000420:Albuterol; C058948:RU 42173