THE PHARMACOLOGICAL ACTIVITY OF 4-KETOAMYLTRIMETHYLAMMONIUM IODIDE AND 3-KETOBUTYLTRIMETHYLAMMONIUM IODIDE

¹ Department of Pharmacology, West Virginia University School of Medicine, Morgantown

1. 4-Ketoamyltrimethylammonium iodide, 3-ketobutyltrimethylammonium iodide, ethoxyethyltrimethylammonium iodide, and amyltrimethylammonium iodide have been compared with acetylcholine for effects on the cardiovascular systems of the dog and rabbit, on isolated rabbit intestine, on rabbit pupil, and for toxicity in mice.

2. All of the agents have less effect on the cardiovascular system of the anesthetized dog and rabbit than acetylcholine, although the ethoxyethyltrimethylammonium and amyltrimethylammonium approach it in depressor activity. The keto compounds are predominantly nicotinic in action and have much less muscarinic activity. The ketoamyl compound is more active than the ketobutyl.

3. When given subcutaneously, the ketoamyl compound is most toxic for mice, the ethoxyethyltrimethylammonium and amyltrimethylammonium less, the ketobutyl even less toxic, and acetylcholine least toxic.

4. On isolated rabbit intestine, acetylcholine is 10 to 20 times as active as ethoxyethyltrimethylammonium in producing an increase in tone, 25 to 30 times as active as amyltrimethylammonium, 50 to 100 times as active as the 4-ketoamyltrimethylammonium, and 100 to 200 times as active as the 3-ketobutyltrimethylammonium.

5. One per cent solutions of the amyltrimethylammonium and ethoxyethyltrimethylammonium iodides produce miosis in the rabbit when applied topically. The other agents do not have this effect at twice this concentration.

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