2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  3. GABA Receptor Sodium Channel Cytochrome P450
  4. Denzimol hydrochloride

Denzimol hydrochloride is an orally active anticonvulsant agent. Denzimol hydrochloride inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol hydrochloride selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol hydrochloride can be used for the research of epilepsy and convulsions.

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Denzimol hydrochloride

Denzimol hydrochloride Chemical Structure

CAS No. : 77234-90-3

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Denzimol hydrochloride Related Antibodies

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Description

Denzimol hydrochloride is an orally active anticonvulsant agent. Denzimol hydrochloride inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol hydrochloride selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol hydrochloride can be used for the research of epilepsy and convulsions[1][2][3][4][5][6].

In Vitro

Denzimol hydrochloride binds reversibly to rat liver microsomal cytochrome P450 as a type II ligand with a Ks value of 6.66 mM[1].
Denzimol (10-10-10-4 M; 20 min) hydrochloride inhibits rat liver microsomal Carbamazepine (HY-B0246) 10,11-epoxidation, Diazepam C3-hydroxylation, and Diazepam N1-dealkylation with IC50 values of 4.26 × 10-7 M, 1.44 × 10-6 M, and 6.66 × 10-7 M, respectively[1].
Denzimol hydrochloride does not alter the plasma protein binding of diazepam in pooled rat serum in vitro[2].

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

Denzimol hydrochloride Related Antibodies
In Vivo

Denzimol (0.94-15 mg/kg; p.o.; single dose) hydrochloride inhibits hepatic drug metabolism in rats[1].
Denzimol (5 mg/kg; p.o.; single dose; 15 minutes prior to Diazepam injection) hydrochloride significantly increases diazepam plasma and brain concentrations in rats by reducing diazepam's total plasma clearance by ~40%, resulting in an 1.8-fold higher plasma AUC0-t and doubled brain diazepam concentrations[2].
Denzimol (up to 289 mg/kg; i.p.; single dose) hydrochloride selectively antagonizes tonic components of Metrazol-induced seizures in rats, with an ED50 of 2.02 mg/kg for protection against tonic hindpaw extension, and shows no activity against clonic seizures at doses up to 260 mg/kg[4].
Denzimol (up to 182 mg/kg; p.o.; single dose) hydrochloride selectively antagonizes tonic components of Metrazol-induced seizures in mice, with an ED50 of 8.8 mg/kg for protection against tonic hindpaw extension, and shows no activity against clonic seizures at doses up to 182 mg/kg[4].

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

Animal Model: CD-COBS rats (male, 200-300 g)[1]
Dosage: 15 mg/kg (CBZ disposition study); 0.94, 1.87, 3.75, 7.50, 15.0 mg/kg (pentobarbitone sleeping time study)
Administration: p.o.; single dose; 30 minutes before CBZ injection (CBZ disposition study); p.o.; single dose; 1 hour before pentobarbitone injection (pentobarbitone sleeping time study)
Result: Reduced CBZ total plasma clearance from 15.3 mL/min/kg to 9.9 mL/min/kg.
Prolonged CBZ elimination half-life from 83 minutes to 134 minutes.
Caused non-significant increase in CBZ-E elimination half-life from 184 minutes to 240 minutes.
Caused non-significant reductions in CBZ-E peak plasma concentrations from 14 nmol/mL to 11 nmol/mL and time to maximum CBZ-E concentrations from 132 minutes to 202 minutes.
Prolonged pentobarbitone sleeping time.
Achieved an ED50 of 3.0 mg/kg for doubling or more of control sleeping time.
Animal Model: CD-COBS (male, 270-300 g)[2] 5 mg/kg
Dosage: 5 mg/kg
Administration: p.o.; single dose; 15 minutes prior to diazepam injection
Result: Increased plasma diazepam concentrations throughout the 180-minute sampling period, resulting in a 1.8-fold increase in plasma area under the curve (AUC).
Reduced total plasma clearance of diazepam by ~40%.
Doubled diazepam brain concentrations compared to controls at both 60 minutes and 180 minutes.
Had no significant effect on diazepam's apparent volume of distribution, elimination half-life, or plasma protein binding.
Animal Model: Sprague-Dawley (female, 110-130 g, maximal metrazol/PTZ-induced seizures model)[4]
Dosage: up to 289 mg/kg
Administration: i.p.; single administration
Result: Achieved an ED50 of 2.02 mg/kg for protection against tonic hindpaw extension.
Achieved an ED50 of 22.5 mg/kg for protection against tonic forepaw extension.
Showed no measurable ED50 for protection against twitches/tremors or clonic seizures at doses tested.
Achieved an ED50 of 289 mg/kg for induction of ataxia.
Animal Model: Sprague-Dawley (female, 110-130 g, maximal metrazol/PTZ-induced seizures model)[4]
Dosage: up to 182 mg/kg
Administration: p.o.; single dose
Result: Achieved an ED50 of 8.8 mg/kg for protection against tonic hindpaw extension.
Achieved an ED50 of 20.2 mg/kg for protection against tonic forepaw extension.
Showed no measurable ED50 for protection against twitches/tremors or clonic seizures at doses tested.
Achieved an ED50 of 146.1 mg/kg for induction of ataxia.
Molecular Weight

328.84

Formula

C19H21ClN2O
CAS No.
SMILES

OC(C1=CC=C(CCC2=CC=CC=C2)C=C1)CN3C=CN=C3.Cl
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Purity & Documentation
References
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Denzimol hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Denzimol77234-90-3GABA ReceptorSodium ChannelCytochrome P450Gamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorNa channelsNa+ channelsCYPsdiazepamepilepsycarbamazepineratsrat liver microsomesphenytoinbenzodiazepine receptorsrat liver cytochrome P450miceconvulsionsInhibitorinhibitorinhibit

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