2. Metabolic Enzyme/Protease Neuronal Signaling
  3. Carboxylesterase (CES) Cholinesterase (ChE)
  4. Heptenophos

Heptenophos is an inhibitor of AChE and plasma carboxylesterase (CES). By inhibiting AChE activity, Heptenophos causes the accumulation of acetylcholine at cholinergic synapses, thereby triggering typical symptoms of organophosphate poisoning. Heptenophos exhibits rapid lethal toxicity in male albino mice, but its toxic effects are effectively antagonized by obidoxime, and Memantine (HY-B0591) further enhances the detoxification efficacy of obidoxime. Therefore, Heptenophos is commonly used in studies related to the mechanism of organophosphate poisoning and detoxification strategies.

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Heptenophos

Heptenophos Chemical Structure

CAS No. : 23560-59-0

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Heptenophos Related Antibodies

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Description

Heptenophos is an inhibitor of AChE and plasma carboxylesterase (CES). By inhibiting AChE activity, Heptenophos causes the accumulation of acetylcholine at cholinergic synapses, thereby triggering typical symptoms of organophosphate poisoning. Heptenophos exhibits rapid lethal toxicity in male albino mice, but its toxic effects are effectively antagonized by obidoxime, and Memantine (HY-B0591) further enhances the detoxification efficacy of obidoxime. Therefore, Heptenophos is commonly used in studies related to the mechanism of organophosphate poisoning and detoxification strategies[1][2].

IC50 & Target

AChE

 

In Vivo

Heptenophos (1.3 LD50; intravenous injection; single administration) strongly inhibits central, peripheral and erythrocyte AChE as well as plasma CES in male albino mice, with an intravenous LD50 of 196.68 μmol/kg. In contrast, Trimedoxime (HY-165600A) exerts time-dependent protective efficacy in Heptenophos-poisoned mice, with an ED50 of 14.66 μmol/kg, and can reactivate brain and diaphragm AChE as well as plasma CES[1].
The intravenous LD50 of Heptenophos in male albino mice is 196.68 μmol/kg. When administered in combination, obidoxime chloride (HY-W011108) at an ED50 of 21.56 μmol/kg is required to achieve a 50% survival rate (Heptenophos at 1.3 LD50; intravenous injection; single administration)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: albino mice (male, 18-24 g)[1]
Dosage: 1.3 LD50; 196.68 μmol/kg (LD50)
Administration: i.v.; single dose
Result: Induced severe inhibition of central, peripheral, and erythrocyte AChE as well as plasma carboxylesterase, leaving 3.33% of erythrocyte AChE, 3.37% of brain AChE, 13.05% of diaphragmal AChE, and 7.3% of plasma carboxylesterase activity uninhibited.
Reached an intravenous LD50 of 196.68 μmol/kg (95% confidence interval: 163.72-208.41).
Animal Model: Albino mice (male, 18-24 g)[2]
Dosage: 1.3 LD50 (toxic challenge); 196.68 μmol/kg (LD50 determination)
Administration: i.v.; single dose
Result: Determined an intravenous LD50 of 196.68 μmol/kg (95% confidence interval: 163.72-208.41 μmol/kg).
Required an obidoxime ED50 of 21.56 μmol/kg to achieve 50% survival when administered concurrently with 1.3 LD50 heptenophos.
Molecular Weight

250.61

Formula

C9H12ClO4P
CAS No.
SMILES

O=P(OC1=C(Cl)C2C=CCC12)(OC)OC
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Purity & Documentation
References
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Heptenophos Related Classifications

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Keywords:

Heptenophos23560-59-0Carboxylesterase (CES)Cholinesterase (ChE)CarboxylesteraseCarboxylic-ester Hydrolaseerythrocyte AChEobidoximecholinergic synapsesmiceorganophosphate poisoningacetylcholinesterasemale Albino micetrimedoximememantineplasma carboxylesteraseInhibitorinhibitorinhibit

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