Add time:09/27/2019         Source:sciencedirect.com

Amidephrine, a phenethanolamine with a methylsulfonamido radical at them-position on the benzene ring, exhibited sympathomimetic effects attributable to selective stimulation of the adrenergic α-receptor. The effects included (1) high affinity for isolated tissues classically identified as prominent α-receptor sites and complete blockade of the amidephrine-evoked responses of these tissues by phentolamine, (2) pronounced ineffectiveness on isolated tissues populated chiefly with ß-receptors, (3) potent mydriatic action in the rabbit and selective antagonism of this effect by phentolamine and (4) potent stimulant action on the smooth muscle of the cat nictitating membrane, the latter action not affected significantly by short-term reserpine pretreatment or by chronic postganglionic denervation. Amidephrine did not show anti-histaminic, cholinergic, anticholinergic or local anesthetic actions.Certain properties can be attributed to the methylsulfonamido substituent of amidephrine as defined by departures from the pharmacologic activity of its hydroxy substituted counterpart, phenylephrine. Particularly, these properties are (1) increased potency and duration of α-receptor stimulant action (2) decreased ß-receptor stimulant action (3) emergence of weak ß-receptor blocking action (4) lessened acute irritant effects on mucous membranes and cutaneous tissue and (5) species dependent changes in acute lethal effect.

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