96750-66-2

Chlorisondamine is an antagonist of nicotinic acetylcholine receptors (nAChRs; IC₅₀ = 1.8 μM in rat striatal synaptosomes) and a ganglion blocker. 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. 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. 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.

Chlorisondamine diiodide has been used:

• as a nicotinic receptor antagonist to test its effect on trinitrobenzene sulfonic acid (TNBS)-induced colitis
• as an irreversible nicotinic acetylcholine(nAChR) blocker to pre-treat brain samples to test its effect on cytochrome P450 2B (CYP2B) induction
• as a ganglionic blocker to test its effect on regulating corticosterone levels in rat with chronic stress

Chlorisondamine diiodide mediates ganglionic and central blockade.

[1] H. EL-BIZRI  P. B S C. Blockade of nicotinic receptor-mediated release of dopamine from striatal synaptosomes by chlorisondamine and other nicotinic antagonists administered in vitro[J]. British Journal of Pharmacology, 1994, 111 2: 406-413. DOI: 10.1111/j.1476-5381.1994.tb14749.x
[2] CLARKE P B. Chronic central nicotinic blockade after a single administration of the bisquaternary ganglion-blocking drug chlorisondamine.[J]. British Journal of Pharmacology, 1984, 83 2: 527-535. DOI: 10.1111/j.1476-5381.1984.tb16517.x
[3] C. REAVILL. Chlorisondamine blocks acquisition of the conditioned taste aversion produced by (?)-nicotine[J]. Neuropharmacology, 1986, 25 9: Pages 1067-1069. DOI: 10.1016/0028-3908(86)90204-2
[4] A J PLUMMER. Ganglionic blockade by a new bisquaternary series, including chlorisondamine dimethochloride.[J]. Journal of Pharmacology and Experimental Therapeutics, 1955, 115 2: 172-184.