Cholinolytic action phencyclidine derivatives

The cholinolytic activity of the hallucinogenic drug, phencyclidne (Sernyl^®) was studied on the isolated frog rectus abdominis muscle. Direct interaction of phencyclidine derivatives with the cholinoceptor was shown to be based on their having a molecular structure and reactivity pattern similar to that of acetylcholine. Phencyclidine is also a very potent inhibitor of butrylcholine esterase. In the frog rectus abdominis, the preponderant enzyme is acetylcholine esterase which is more resistant to phencyclidine and therefore is more suited to asay the drug action on the cholinoceptor. The relations between the structure of the molecule and ACh is discussed on the basis of quantum mechanics.