Ro 21-7634, a new antiallergic agent with potent oral activity.
Ro 21-7634 was examined for oral antiallergic activity in two in vivo models commonly used to evaluate antiallergics. In the rat PCA test, this drug had an oral ID50 of 1.14 mg/kg and was found to be more potent than several other antiallergics including Disodium Cromoglycate (cromoglycate), Oxatomide, Doxanthrazole, Xanoxate, 2,6-bis (ethyoxyoxalylamino) pyridine, PRD-92-EA and M + B 22,948. In contrast to cromoglycate, Ro 21-7634 was found to be an orally active inhibitor of antigen-induced broncho-constriction in passively sensitized rats (ID50 = 0.2 mg/kg). In addition, Ro 21-7634 inhibited antigen-induced histamine release in an in vivo passive peritoneal anaphylaxis test system, following intraperitoneal administration. Ro 21-7634 demonstrated no end organ antagonism toward histamine, metacholine or serotonin in the guinea pig.
D000284:Administration, Oral; D000818:Animals; D006168:Guinea Pigs; D006633:Histamine Antagonists; D006967:Hypersensitivity / Q000188:drug therapy*; D007112:Immunity, Maternally-Acquired / Q000187:drug effects; D008297:Male; D016210:Methacholine Chloride; D008688:Methacholine Compounds / Q000037:antagonists & inhibitors; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D011725:Pyridines / Q000627:therapeutic use*; D011799:Quinazolines / Q000627:therapeutic use*; D051381:Rats; D011919:Rats, Inbred Strains; D012702:Serotonin Antagonists
D006633:Histamine Antagonists; D008688:Methacholine Compounds; D011725:Pyridines; D011799:Quinazolines; D012702:Serotonin Antagonists; D016210:Methacholine Chloride; C023625:2-methoxy-11-oxo-11H-pyrido(2,1-b)quinazoline-8-carboxylic acid