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Cat. No. Name Size Price Add Cart
KI0804Chlorprothixene50 mg$154

Chemical Characteristic

Product NameChlorprothixene
SynonymsTaractan
CAS No.113-59-7
Molecular Weight 315.86
FormulaC18H18ClNS
Chemical Name3-(2-Chlorothioxanthen-9-ylidene)-N,N-dimethyl-propan-1-amine
SmilesC(C/C=C\1/c2cc(ccc2Sc2ccccc12)Cl)N(C)C
Chemical Structure

Biological activities

Chlorprothixene is a neuroleptic drug. Chlorprothixene has tranquillizing and thymoleptic activities.[1] Chlorprothixene is also a potent antagonist of NA-induced contractions of denervated nictitating membranes.[2] Chlorprothixene inhibits the 3H-GABA uptake with an IC50 ranging from 10 to 30 µM.[3] Chlorprothixene selectively inhibits histamine-induced calcium release with an IC50 of 1 nM.[4] High dose of chiorprothixene inhibits the protection afforded by iproniazid against the reserpine-induced release of catecholamines in adrenal medulla and brain as well as the decrease of 5HT (5HT) and catecholamines. Chlorprothixene can antagonize the accumulation of 5-hydroxytryptamine and norepinephrine (NE) which is caused by iproniazid. Chlorprothixene can act by decreasing the permeability of the storage organelles for some monoamines (5HT, DA).[5] Chlorprothixene exhibits a rather good antagonism of noradrenaline and dopamine. The increases in the toxicity of yohimbine hydrochloride (20 mg/kg subcutaneously) in mice caused by chlorprothixene.[6]

Protocols

Chlorprothixene is dissolved in aqueous solution. [3]

References

[1] Scanlan EP, et al. A controlled trial of taractan in chronic schizophrenia. Br J Psychiatry. 1963, 109: 418-421.
[2] Fjalland B, et al. Neuroleptic blockade of the effect of various neurotransmitter substances. Acta Pharmacol Toxicol (Copenh). 1978, 42(3): 206-211.
[3] Fjalland B. Inhibition by neuroleptics of uptake of 3H-GABA into rat brain synaptosomes. Acta Pharmacol Toxicol (Copenh). 1978, 42(1): 73-76.
[4] Vasudevan SR, et al. Shape-based reprofiling of FDA-approved drugs for the H? histamine receptor. J Med Chem. 2012, 55(16): 7054-7060.
[5] GEY KF, et al. Influence of chlorpromazine and chlorprothixene on the cerebral metabolism of 5-hydroxytryptamine, norepinephrine and dopamine. J Pharmacol Exp Ther. 1961, 133: 18-24.
6] Quinton RM. The increase in the toxicity of yohimbine induced by imipramine and other drugs in mice. Br J Pharmacol Chemother. 1963, 21: 51-66.

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