The uptake kinetics and metabolism of extraneuronal noradrenaline in guinea-pig trachea as studied with quantitative fluorescence microphotometry.

1 Extraneuronal uptake of noradrenaline and alpha-methylnoradrenaline into single cells of guinea-pig tracheal smooth muscle have been studied by means of quantitative fluorescence microphotometry. 2 Fluorescence brightness due to accumulation of alpha-methylnoradrenaline was dose-dependent and was increased by the catechol-O-methyltransferase inhibitor drugs, tropolone or beta-thujaplicin (200 micrometer) but not by 3,4-dimethoxy-5-hydroxybenzoic acid (200 microgram). 3 Fluorescence brightness due to accumulation of noradrenaline was increased if animals were pretreated with the monoamine oxidase inhibitor drug, nialamide. 4 The study suggests that metabolism of amines by catechol-O-methyltransferase and monoamine oxidase can occur subsequent to extraneuronal uptake is guinea-pig tracheal smooth muscle. 5 The uptake of noradrenaline into tracheal smooth muscle was concentration-dependent, saturable, and had a Km of 156 micrometer.