U-101017  (Synonyms: PNU 101017)

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

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 K_i of 3.37±0.22 nM^[2].

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

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].

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

442.94

C₂₃H₂₇ClN₄O₃

170568-47-5

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

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• [1]. Hall ED, et al. Comparative neuroprotective properties of the benzodiazepine receptor full agonist diazepam and the partial agonist PNU-101017 in the gerbil forebrain ischemia model. Brain Res. 1998 Jul 6;798(1-2):325-9.  [Content Brief]

  [2]. Sethy VH, et al. The novel anxiolytic U-101017: in vitro and ex vivo binding profile and effect on cerebellar cGMP. Pharmacol Biochem Behav. 1997 Oct;58(2):609-13.  [Content Brief]