Abstract
Isoprenaline, a sympathomimetic drug used in the treatment of asthma, was found to be sulphated by the bronchial tissues of the monkey and dog. Enzyme preparations of the liver, small intestine and kidney of various animals are also able to catalyze this sulphate conjugation reaction from ATP and inorganic sulphate and from a commercial preparation ofadenosine 3'-phosphate 5'-sulphatophosphate (PAP 35S) or PAP 35S generated from Naz 2 35SC 4 in vitro. The K m values for isoprenaline for the sulphotransferase of mouse liver and monkey lung, are respectively, 51.3 μM and 138 μM. The significance of this detoxication reaction is discussed in relation to (a) the importance of lung as a potential biotransformation site of isoprenaline, (b) asthma deaths supposed to be associated with the use of isoprenaline in the form of pressurised aerosols and (c) the ability of the different tissues to synthesize PAPS in vitro.
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