Inhibition of catecholamine Uptake₂ by steroids in the isolated rat heart

Abstract

Various steroids (1 7‐fl‐oestradiol, cortico‐sterone, deoxycorticosterone, progesterone, testosterone and androsterone) produced a dose‐dependent inhibition of the uptake of 3H‐noradrenaline by the Uptake2 mechanism in the isolated perfused heart. It is suggested that these results may explain the potentiating effects of such steroids on the responses of vascular smooth muscle to catecholamines.

Effect of steroids on β‐adrenoceptor‐mediated relaxation of pig bronchus

“…17,B-Oestradiol, progesterone, testosterone, corticosterone, deoxycorticosterone and cortisol-HS are potent inhibitors of extraneuronal catecholamine uptake (Kalsner, 1969;Salt, 1972;Cornish etal., 1978) Of these steroids, only 17p-oestradiol is known also to inhibit the neuronal uptake of catecholamines (Iversen & Salt, 1970;Salt, 1972;Cornish et al, 1978). Normetanephrine (4-22 ElM) is known to inhibit selectively extraneuronal uptake by approximately 50% (Burgen & Iversen, 1965;Mireyless & Foster, 1973;Major, Sauerwein & Graefe, 1978).…”

Inhaled corticosteroids reduce asthma-associated airway hyperperfusion through genomic and nongenomic mechanisms

“…Corticosteroids could increase sympathetic signal transmission and consequently vascular tone by inhibiting extraneuronal catecholamine uptake [33]. This nongenomic mechanism was demonstrated recently in dissociated rabbit aortic smooth muscle cells by showing that the inhibitory action on noradrenaline uptake occurred rapidly, was neither altered by protein synthesis nor transcription inhibitors, and could be reproduced with a corticosteroid made membrane-impermeant by conjugation to bovine serum albumin [34].…”

An Inhibitor of Cerebral Uptake of Noradrenaline in Jaundiced Blood Plasma

“…Among possible candidates are certain steroid hor mones and cholesterol. Several estrogens, gluco corticoids, and progesterone inhibit uptake-2 in rat heart and in arterial smooth muscle (Iversen and Salt, 1970;Nicol and Rae, 1972). Cholesterol is an inhibitor of lower affinity (Salt and Iversen, 1972) but is present in plasma at an appropriately higher concentration.…”