Oxatomide structure

Finally, in this context we should watch closely the clinical development of compounds of a type not covered in this introduction. These are basic compounds, structurally more similar to histamine Hi-antagonists, which inhibit mediator release but which are also potent physiological or competitive antagonists ketotifen, from Sandoz, and oxatomide from Janssen are two recent examples of this type of compound. 

Mediator release inhibitors with antihistamine activity Several agents which are both antihistamines and inhibitors of mediator release have also been reported (Figure 12). An early compound of this type was Schering 15,280 (C, azanator) (76). Three other compounds (Cl, Cll and ClII) have subsequently been reported (TJ-SI). The most advanced of these is ketotifen (Cl) which is structurally related to azanator. It is orally active in man at 1 mg (b.i.d.) (Z7) and has been marketed by Sandoz in Switzerland. Two other potent, orally active compounds in the rat PCA procedure are Janssen s oxatomide (7 ,79) and Boehringer Mannheim s BM 15,100 (S0>S1)- These compounds combine the properties of mediator release inhibition with antihistamine activity. 

Introduction. Oxatomide and analogous structures were synthesized as a part of an extensive chemical research project. 

Morphological Studies. The methods used to study peribronchiolar mast cells at the ultra structural level have been fully described (1 7, 18). Specimens were obtained from sensitized non-challenged guinea-pigs, and from control or oxatomide-treated animals 3 min after the injection of ovalbumin. 

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