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Purity: ≥98%
Imepitoin, formerly known as AWD 131-138 and ELB 138, is a novel partial BZD (benzodiazepine) receptor agonist that has the potential use as an antiepileptic drug for the treatment of canine idiopathic epilepsy. Imepitoin is a centrally acting anti-epileptic which crosses the blood brain barrier. It inhibits seizures via potentiation of the GABA a receptor-mediated inhibitory effects on the neurones. Imepitoin exerts significant anticonvulsant efficacy without tolerance in a dog seizure model as well as in epileptic dogs with spontaneously recurrent seizures. These data thus substantiate that partial agonism at the BZD site of GABAA receptors offers advantages versus full agonism and constitutes a valuable approach for treatment of seizures.
| ln Vitro |
Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2, and alpha5beta2gamma2) were dose-dependently stimulated GABA currents by AWD 131–138. This allosteric stimulation amounted, on average, to roughly 12–21% of the maximal stimulation attained with diazepam at 10 microM AWD 131–138. The stimulation threshold ranged from 0.3 to 1.0 microM [1].
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| ln Vivo |
At cumulative doses up to 18.0 mg/kg im (plasma levels over 2100 ng/ml), AWD 131–138 did not change response rates or cause midazolam-like responding. Within three sessions of studying AWD 131-138 (10-100 microg/kg/injection) by substitution, responding decreased to vehicle substitution levels. Sufficient drug was self-administered during the first session (approximately 3.5 mg/kg) at the dose of 100 microg/kg iv AWD 131-138 to produce plasma levels above 1000 ng/ml; however, responding dropped to vehicle levels over the next two sessions [2]. In the PTZ dog model, prolonged oral administration of ELB 138 at twice-daily doses of either 5 or 40 mg/kg for a duration of 5 weeks was not linked to a decrease in the drug's anticonvulsant efficacy [3].
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| References |
[1]. Sigel E, et al. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site. Neurosci Lett. 1998 Apr 3;245(2):85-8.
[2]. Yasar S, et al. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. Eur J Pharmacol. 2003 Apr 4;465(3):257-65. [3]. Loscher W, et al. Anticonvulsant efficacy of the low-affinity partial benzodiazepine receptor agonist ELB 138 in a dog seizure model and in epileptic dogs with spontaneously recurrent seizures. Epilepsia. 2004 Oct;45(10):1228-39. |
| Molecular Formula |
C13H14CLN3O2
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| Molecular Weight |
279.08
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| CAS # |
188116-07-6
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])N1C(N=C(C1([H])[H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5832 mL | 17.9160 mL | 35.8320 mL | |
| 5 mM | 0.7166 mL | 3.5832 mL | 7.1664 mL | |
| 10 mM | 0.3583 mL | 1.7916 mL | 3.5832 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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