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Ethopropazine is a butyrylcholinesterase (BChE) inhibitor (IC50 = 15.14 µM in human erythrocyte lysates).1 It is selective for BChE over acetylcholinesterase (AChE) at 500 µM. Ethopropazine also binds to rat forebrain and hindbrain membrane preparations (Kis = 3.1 and 7.2 nM, respectively), which are endogenously enriched in M1 and M2 muscarinic acetylcholine receptors, respectively.2 Ethopropazine (0.232 mg/kg) decreases the intensity and increases the latency of haloperidol-induced catalepsy, a model of extrapyramidal syndrome, in rats when used in combination with the adenosine A2A receptor antagonist ZM 241395 (Item No. 20447).3 It reduces thermal hyperalgesia in a rat model of neuropathic pain induced by sciatic nerve ligation when administered at doses of 20 and 30 mg/kg.4 Formulations containing ethopropazine were previously used in the treatment of Parkinson’s disease.
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1. 1-
2. The relative selectivity of anticholinergic drugs for the M1 and M2 muscarinic receptor subtypes. Mov. Disord. 1(2), 135-144 (1986).
3. Synergism of theophylline and anticholinergics to inhibit haloperidol-
4. Anti-