A BChE inhibitor (IC50 = 15.14 µM in human erythrocyte lysates); selective for BChE over AChE at 500 µM; binds to rat forebrain and hindbrain membrane preparations (Kis = 3.1 and 7.2 nM

Ethopropazine (hydrochloride) – 25 mg

Brand:
Cayman
CAS:
1094-08-2
Storage:
-20
UN-No:
Non-Hazardous - /

Ethopropazine is a butyrylcholinesterase (BChE) inhibitor (IC50 = 15.14 µM in human erythrocyte lysates).{53481} 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.{53482} 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).{53483} 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.{53484} Formulations containing ethopropazine were previously used in the treatment of Parkinson’s disease.  

 

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Description

A BChE inhibitor (IC50 = 15.14 µM in human erythrocyte lysates); selective for BChE over AChE at 500 µM; 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; decreases the intensity and increases the latency of haloperidol-induced catalepsy, a model of extrapyramidal syndrome, in rats when used in combination with ZM 241395 at 0.232 mg/kg; reduces thermal hyperalgesia in a rat model of neuropathic pain induced by sciatic nerve ligation at 20 and 30 mg/kg

Formal name: N,N-diethyl-α-methyl-10H-phenothiazine-10-ethanamine, monohydrochloride

Synonyms:  NSC 169467|NSC 64074

Molecular weight: 348.9

CAS: 1094-08-2

Purity: ≥98%

Formulation: A solid

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