The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
本发明提供了一种非去极化型的神经肌肉阻滞剂,其循环效应很少或没有。该发明的化合物包括
富马酸、
马来酸、
琥珀酸和
乙炔二
羧酸的双(
异喹啉基烷醇)二酯;适用于这些化合物的静脉注射制剂作为麻醉手术辅助剂,以及制备这些化合物的方法。该发明的化合物可以产生短期或中等期的神经肌肉阻滞效果,对于各种化合物,可以通过给予巯基化合物如
L-半胱氨酸、
D-半胱氨酸或
谷胱甘肽来逆转。对于该发明的各种化合物,神经肌肉阻滞效果可以快速、有效地逆转,且没有明显的副作用。