Some actions of 4,17a-dimethyl-4,17a-diaza-D-homo-5α-androstane dimethiodide (HS-342), a new neuromuscular blocking drug

Abstract

Abstract The effects of the newly-synthesized bisquaternary steroid 4,17a-dimethyl-4,17a-diaza-D-homo-5α-androstane dimethiodide (HS-342) have been investigated on the rat isolated phrenic nerve-hemidiaphragm, chick biventer cervicis and intact cat tibialis anterior muscle preparations, on the guinea-pig isolated ileum and on the rat isolated vas deferens preparations. The anticholinesterase activity of HS-342 was also measured. In the skeletal muscle preparations HS-342 exhibited properties of a post-junctionally active neuromuscular blocking agent of the non-depolarizing class. In the anaesthetized cat HS-342 exhibited approximately equal activity to that of tubocurarine, but its duration of action was about one-third of that of tubocurarine. HS-342 exhibited low anticholinesterase activity, low muscarinic blocking activity and apparently had no effect on the adrenergic neuroeffector junction studied.