2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. ENX-101

ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.

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ENX-101 Chemical Structure

ENX-101 Chemical Structure

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ENX-101 Related Antibodies

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Description

ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models[1].

In Vitro

ENX-101 (0.01 nM-10 μM) potently enhances currents generated by GABA in receptors containing α2,α3,α5 subunits but causes negligible potentiation ofα1 subunit-containing receptors in Chinese hamster ovary (CHO) cells[1].

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

ENX-101 Related Antibodies
In Vivo

ENX-101 (30-300 mg/mL, i.p., a single dose 0.25 h prior to challenge with current) in outbred adult male CF-1 mice (20-35 g) model protects most animals stimulated at 32 mA but fewer animals at 44mA[1].
ENX-101 (1-100 mg/kg, p.o., a single dose 2 h prior to electrical stimulation) significantly inhibits the behavioral seizure response and reduces the mean afterdischarge duration in both amygdala and the cortex in a dose-dependent manner with amygdala kindled seizure rat model[1].
ENX-101 (0.075-100 mg/kg, p.o., a single dose) significantly reduces the overall spike-and-wave discharge (SWD) during the post-treatment observation period (10-130 min) in male Wistar Genetic Absence Epilepsy Rat from Strasbourg (GAERS) rats[1].
ENX-101 (10-100 mg/kg, p.o., a single dose) did not cause motor impairments at anti-seizure doses in rat models[1].

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

Animal Model: Amygdala kindled seizure rat model [1]
Dosage: 1 mg/kg, 6 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral gavage (p.o.)
Result: Significantly reduced the mean seizure severity score by -1.8 (p < 0.01), -3.2 (p < 0.001), -3.8 (p < 0.01) respectively.
Reduced mean afterdischarge duration in the cortex (−30%, p < 0.01; −53%, p < 0.01; and −66%, p < 0.001) and amygdala −26% (p < 0.01), −46% (p < 0.01), and −64% (p < 0.001).
Showed greatest reductions in seizure severity score (-4.0) and afterdischarge duration in the cortex (−76%, p < 0.05) and in the amygdala (−78%) with 100 mg/kg but without significance.
Resulted in average plasma exposures of 191, 487, and 1102 ng/mL 2 h after dosing with 1, 6, 30 mg/kg.
Molecular Weight

426.47

Formula

C19H12D9F2N7O2
SMILES

FC1=CC=C(F)C=C1C2=NN=C3N2N=C(OCC4=NC=NN4C)C(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=C3.O
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ENX-101 Related Classifications

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Help & FAQs
  • 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:

ENX-101ENX101ENX 101GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα2α3α5selectiveGABAAreceptorPAMantiseizureInhibitorinhibitorinhibit

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