The ganglionic blocking properties of the cholinesterase reactivator, HS-6

Abstract

rbllowlng i.v. administration of 30 mg/kg of the chol inesterase reactivator HS-6, blood pres7ure fel l (up to 50 nmi/Hg) and maxima l blood levels of HS-6 reached 242~~g/ml . HS-6 attenuated the pressor response resul ting from carotid occlusion and the depressor effect of vagal stimulation . Doses of HS-6 below those tested therapeutically against soman In different anima l species (3.59-lo,77mq/kg) progressively blocked the ganglion stimulati ng effects of nicoti ne and dimethy l phenylpl perazinlum but not those following adrenaline , a pattern similar to that produced by hexamethonium but only 1/84 as potent. HS-6, like hexamethon i um and mecamyl amine, progressively blocked the contraction of the ni cti tating membrane of the cat resulting from pre-gangl ionic stimulation .The results indicate that HS-6 possesses gangl ion bl ocking properties at doses likely to have any value therapeutically In soman poisoning. The ganglion blocking properties of the drug may be a factorIn the beneficial effects of HS-6.

Examination of the Role of Central Cholinergic Mechanisms in the Therapeutic Effects of HI‐6 in Organophosphate Poisoning

“…Other peripheral mechanisms may also play important roles in the effects of oximes of the HI‐6 type. Biological properties of these oximes include ganglionic blockade (Lundy, 1978; Lundy and Tremblay, 1979; Kirsch et al, 1981); hemicholinium‐like and antimuscarinic activity (Kuhnen Clausen, 1972; Clement, 1979 b ; Amitai et al, 1980), together with effects on the diaphragm or intercostal muscles (Wolthius et al, 1981; Clement, 1981).…”