Chlorisondamine (iodide)

Chlorisondamine is an antagonist of nicotinic acetylcholine receptors (nAChRs; IC₅₀ = 1.8 µM in rat striatal synaptosomes) and a ganglion blocker.¹ It decreases dopamine release induced by nicotine (Item Nos. 16535 | 20887) in a dose-dependent manner in rat striatal synaptosomes at concentrations ranging from 0-100 µM. The effect of chlorisondamine is long-lasting, with a 10 mg/kg dose blocking nicotine-induced stimulant activity for at least five weeks.² Chlorisondamine (5 µg, i.c.v.) prevents rats from acquiring a (–)-nicotine-induced conditioned taste aversion response, a model of the aversive effects of nicotine.³ It also inhibits autonomic ganglia, providing approximately 50% inhibition of the contractile response in feline superior cervical ganglion nictitating membrane preparations when administered at a dose of 50 mg/kg.⁴

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1. el-Bizri, H., and Clarke, P.B. Blockade of nicotinic receptor-mediated release of dopamine from striatal synaptosomes by chlorisondamine and other nicotinic antagonists administered in vitro. Br. J. Pharmacol. 111(2), 406-413 (1994).

2. Clarke, P.B. Chronic central nicotinic blockade after a single administration of the bisquaternary ganglion-blocking drug chlorisondamine. Br. J. Pharmacol. 83(2), 527-535 (1984).

3. Reavill, C., Stolerman, I.P., Kumar, R., et al. Chlorisondamine blocks acquisition of the conditioned taste aversion produced by (−)-nicotine. Neuropharmacology 25(9), 1067-1069 (1986).

4. Plummer, A.J., Trapold, J.H., Schneider, J.A., et al. Ganglionic blockade by a new bisquaternary series, including chlorisondamine dimethochloride. J. Pharmacol. Exp. Ther. 115(2), 172-184 (1955).