The mechanism of action of choline acetyl transferase

Acetylcholine (Ach) is synthesised from acetyl-coA and choline in the cytoplasm of autonomic nerve terminals. The final step in the synthesis is catalysed by the enzyme choline acetyltransferase (CAT). Once formed, Ach is transported into and packaged into synaptic vesicles. Moderately potent inhibitors of CAT do exist but they have no therapeutic benefit and this is due in part to the uptake of choline being the rate-limiting step in the synthesis of Ach.

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References

Introduction to autonomic pharmacology. In: Sedative-hypnotic drugs. In: Basic and clinical pharmacology, 8^th edition. Katzung BG. USA: The McGraw Hill Companies, Inc, 2001:75–91.

Neurotransmission. In: Goodman and Gilman’s the pharmacological basis of therapeutics, 10^th edition. Hardman JG, Limbird LE and Goodman Gilman A. USA: The McGraw-Hill Companies Inc, 2001:115–154.