A BChE inhibitor
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Ethopropazine (hydrochloride)

Item No. 28493

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N-diethyl-α-methyl-10H-phenothiazine-10-ethanamine, monohydrochloride
CAS Number
1094-08-2
Synonyms
  • NSC 64074
  • NSC 169467
Molecular Formula
C19H24N2S • HCl
Formula Weight
348.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMF:PBS (pH 7.2) (1:5): 0.16mg/mLDMSO: 5mg/mLEthanol: 5mg/mL
λmax
252 nm
SMILES
CC(N(CC)CC)CN1C2=C(C=CC=C2)SC3=CC=CC=C31.Cl
InChi Code
InChI=1S/C19H24N2S.ClH/c1-4-20(5-2)15(3)14-21-16-10-6-8-12-18(16)22-19-13-9-7-11-17(19)21;/h6-13,15H,4-5,14H2,1-3H3;1H
InChi Key
VXPCQISYVPFYRK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $62

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    25 mg

    $123

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    50 mg

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    100 mg

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    Product Description

    Ethopropazine is a butyrylcholinesterase (BChE) inhibitor (IC50 = 15.14 µM in human erythrocyte lysates).1 It is selective for BChE over acetylcholinesterase (AChE) at 500 µM. Ethopropazine also binds to rat forebrain and hindbrain membrane preparations (Kis = 3.1 and 7.2 nM, respectively), which are endogenously enriched in M1 and M2 muscarinic acetylcholine receptors, respectively.2 Ethopropazine (0.232 mg/kg) decreases the intensity and increases the latency of haloperidol-induced catalepsy, a model of extrapyramidal syndrome, in rats when used in combination with the adenosine A2A receptor antagonist ZM 241395 (Item No. 20447).3 It reduces thermal hyperalgesia in a rat model of neuropathic pain induced by sciatic nerve ligation when administered at doses of 20 and 30 mg/kg.4 Formulations containing ethopropazine were previously used in the treatment of Parkinson’s disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ucar, G., Gokhan, N., Yesilada, A., et al. 1-N-Substituted thiocarbamoyl-3-phenyl-5-thienyl-2-pyrazolines: a novel cholinesterase and selective monoamine oxidase B inhibitors for the treatment of Parkinson’s and Alzheimer’s diseases. Neurosci. Lett. 382(3), 327-331 (2005).

    2. Burke, R.E. The relative selectivity of anticholinergic drugs for the M1 and M2 muscarinic receptor subtypes. Mov. Disord. 1(2), 135-144 (1986).

    3. González-Lugo, O.E., Ceballos-Huerta, F., Jiméenez-Capdeville, M.E., et al. Synergism of theophylline and anticholinergics to inhibit haloperidol-induced catalepsy: A potential treatment for extrapyramidal syndromes. Prog. Neuropsychopharmacol. Biol. Psychiatry 34(8), 1465-1471 (2010).

    4. Jevtovic-Todorovic, V., Meyenburg, A.P., Olney, J.W., et al. Anti-parkinsonian agents procyclidine and ethopropazine alleviate thermal hyperalgesia in neuropathic rats. Neuropharmacology 44(6), 739-748 (2003).