1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. U-101017

U-101017 (Synonyms: PNU 101017)

Cat. No.: HY-19250
Handling Instructions

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.

For research use only. We do not sell to patients.

U-101017 Chemical Structure

U-101017 Chemical Structure

CAS No. : 170568-47-5

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Description

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.

In Vitro

PNU-101017 potentiates GABA-stimulated Cl- currents at low concentrations (<1 μM)[1]. U-101017 concentration-dependently inhibits the binding of [3H]FNZ to the membrane preparation of rat cerebral cortex in vitro with Ki of 3.37±0.22 nM[2].

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

In Vivo

Pre-ischemic treatment with either PNU-101017 significantly protects the CA1 neuronal population, and PNU-101017 reduces the loss to 50%. Delaying PNU-101017 administration until immediately after reperfusion does not reduce the neuroprotective activity[1]. U-101017 (30 μmol/kg, p.o.) time-dependently blocks [3H]FNZ binding to the mouse cerebral cortex. U-101017 dose-dependently decreases the levels of cGMP with ED50s of 260.0 (163-425) and 0.37 (0.12-1.04) in nonstressed and foot shock-stressed mice, respectively. Flumazenil, an antagonist of GABAA receptors, has no significant effect on cGMP in nonstressed mice, but pretreatment with flumazenil significantly blocks U-101017 (10 μmol/kg, p.o.)-induced reductions in cGMP. In stressed mice, flumazenil is ineffective in altering cerebellar cGMP, but pretreatment with these doses of flumazenil significantly (p < 0.01) blocks U-101017-induced attenuation of stress-induced elevations in cGMP[2].

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

Molecular Weight

442.94

Formula

C₂₃H₂₇ClN₄O₃

CAS No.

170568-47-5

SMILES

O=C(C1=C2N(C=N1)C3=C(C=C(Cl)C=C3)C(C(N4C[[email protected]@H](C)N[[email protected]@H](C)C4)=O)=C2)OC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[1]

Three groups of gerbils (N=9-11/group) are treated i.p. with either vehicle (0.05 N HCl), PNU-101017 (30 mg/kg) or diazepam (10 mg/kg) 30 min prior to ischemia and again 2 h after reperfusion. Two other groups receive PNU-101017 or diazepam immediately after reperfusion and again 2 h later. The tested doses of PNU-101017 and diazepam are selected from past studies demonstrating their neuroprotective efficacy in the gerbil forebrain ischemia model. The administration of the second dose at 2 h after reperfusion is consistent with previous dosing with other effective compounds tested in the gerbil. The 0.05 N HCl vehicle has been employed for i.p. dosing with other test compounds and is devoid of toxicity or acute distress production.

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

References
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Keywords:

U-101017PNU 101017U101017U 101017PNU101017PNU-101017GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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