PHARMACOLOGIC PROPERTIES OF ANTRENYL (OXYPHENONIUM) (BA-5473) DIETHYL(2-HYDROXYETHYL)METHYLAMMONIUM BROMIDE -PHENYL-CYCLOHEXANEGLYCOLATE, AN ANTICHOLINERGIC AGENT

¹ Research Department, Ciba Pharmaceutical Products, Inc., Summit, N. J.

1. Antrenyl is a rapidly absorbed and chemically stable orally active anticholinergic agent with an antispasmodic potency on visceral smooth muscle comparable to atropine. A persistent block of the effects of acetylcholine, methacholine and vagal stimulation is produced after oral and parenteral administration of Antrenyl.

2. Antrenyl possesses less marked mydriatic and antisalivary activity than atropine. Antrenyl blocked salivation induced by methacholine, histamine, and chorda tympani faradization, but not that produced by epinephrine.

3. Antrenyl is capable of blocking transmission in sympathetic ganglia and of impeding myoneural conduction, but only when relatively large amounts are administered intravenously.

4. The acute toxicity of Antrenyl in the rat by several routes of administration and the chronic, three-months oral toxicity in the dog are both of a low order.

5. The specificity of the intestinal spasmolytic action of Antrenyl is indicated by the several thousand-fold concentrations required to prevent barium and histamine-induced contractions of the isolated ileum of the guinea pig.