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Derquantel , a spirocyclic anthelmintic, is a competitive, orally active nicotinic acetylcholine receptor (nAChR) antagonist. Derquantel inhibits ACh-induced depolarization with an IC50 of 0.22 μM. By selectively antagonizing nAChRs on the somatic muscles of nematodes, Derquantel causes flaccid paralysis of muscles, thereby dislodging parasites from the host's gastrointestinal tract. Derquantel is applicable to research related to Haemonchus contortus infection and Ascaris suum infection.

Derquantel (1 μM) is a competitive antagonist of acetylcholine-induced contraction in the body muscle strips of Ascaris suum, altering the EC₅₀ of acetylcholine from 7 μM to 52 μM .
Derquantel (0.1-30 μM; 0-4 min) effectively and reversibly inhibits acetylcholine-induced depolarization in pig roundworm body wall muscle flap preparations, with an IC₅₀ of 200 nM, acting as a competitive antagonist.
Derquantel (1 μM; 30 min) altered the EC₅₀ of acetylcholine in pig roundworm body muscle flap specimens from 4.5 μM to 10.2 μM and reduced the maximum depolarization response, consistent with competitive antagonism.

The combined use of derquantel (2 mg/kg; oral; single dose) and avermectin showed limited efficacy in sheep infected with highly multidrug-resistant Haemonchus contortus.

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