GANGLIONIC BLOCKADE BY A NEW BISQUATERNARY SERIES, INCLUDING CHLORISONDAMINE DIMETHOCHLORIDE

¹ Research Department, Ciba Pharmaceutical Products, Inc., Summit, New Jersey

A series of bisquaternary tetrachloroisoindolines has been found to possess ganglionic blocking activity.

The pharmacology of 4,5,6,7-tetrachloro-2-diethylaminoethyl)-isoindoline dimethochloride (chlorisondamine dimethochloride), the most active of the series, has been presented.

Chlorisondamine dimethochloride is a long-acting, orally effective, specific ganglionic blocking agent of high potency.

In the cat superior cervical ganglion-nictitating membrane preparation, chlorisondamine dimethochloride is approximately six times as active as hexamethonium and twice as active as pentapyrrolidinium in producing ganglionic blockade.

Chlorisondamine dimethochloride shows a rapid onset and prolonged period of maximum effect on the nictitating membrane of the anesthetized dog when given orally. Chlorination of the aromatic ring appears to be important for these properties.

No evidence of toxicity has been noted in dogs during a four-month period of chlorisondamine dimethochloride administration in daily oral doses up to 20 mgm./kgm.