CHLORISONDAMINE DIIODIDE

CHLORISONDAMINE DIIODIDE Property

storage temp. 

2-8°C

solubility 

H₂O: ~3.75 mg/mL

form 

solid

color 

white

Water Solubility 

Soluble to 10 mM in water

Safety

Hazard Codes 

Xn,N

Risk Statements 

22-50

Safety Statements 

60-61

RIDADR 

UN 3077 9 / PGIII

WGK Germany 

2

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

CHLORISONDAMINE DIIODIDE Chemical Properties,Usage,Production

Description

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.

Uses

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

Biochem/physiol Actions

Chlorisondamine diiodide mediates ganglionic and central blockade.

in vivo

References

[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.