VU 29 - CAS 890764-36-0
Category: Inhibitor
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Molecular Formula:
C22H16N4O3
Molecular Weight:
384.39
COA:
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Targets:
mGluR
Description:
VU 29 is a potent positive allosteric potentiator at the rat mGlu5 receptor (EC50 = 9 nM) with selectivity for mGlu5 over mGlu1 and mGlu2 receptors (EC50 = 557 nM and 1.51 μM for mGlu1 and mGlu2, respectively). VU 29 binds to the MPEP allosteric site (Ki app = 244 nM). VU 29 was shown to potentiate both DHPG-induced LTP and threshold θ-burst stimulation (TBS)-induced LTP in rat hippocampal slices.
Brife Description:
positive allosteric potentiator at the rat mGlu5 receptor
Purity:
≥99% by HPLC
Synonyms:
N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide; DPAP; VU-29; VU 29; VU29; 4-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide
MSDS:
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InChIKey:
KIALCSMRIHRFPL-UHFFFAOYSA-N
InChI:
InChI=1S/C22H16N4O3/c27-22(17-11-13-19(14-12-17)26(28)29)23-21-15-20(16-7-3-1-4-8-16)24-25(21)18-9-5-2-6-10-18/h1-15H,(H,23,27)
Canonical SMILES:
C1=CC=C(C=C1)C2=NN(C(=C2)NC(=O)C3=CC=C(C=C3)[N+](=O)[O-])C4=CC=CC=C4
1.Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Impairment of Novel Object Recognition Induced by Acute Ethanol and Ethanol Withdrawal in Rats.
Marszalek-Grabska M;Gibula-Bruzda E;Bodzon-Kulakowska A;Suder P;Gawel K;Filarowska J;Listos J;Danysz W;Kotlinska JH Neurotox Res. 2018 Apr;33(3):607-620. doi: 10.1007/s12640-017-9857-z. Epub 2018 Jan 2.
Glutamate is essential for learning and memory processes, and acute and chronic exposures to ethanol (or protracted abstinence) alter glutamatergic transmission. In the current study, we investigated the effects of VU-29, positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor, on the acute ethanol- and ethanol withdrawal-induced impairment of novel object recognition (NOR) task in rats. The influence of VU-29 (30 mg/kg) on memory retrieval was measured (a) at 4-h delay after acute ethanol administration, as well as (b) after acute withdrawal (24 and 48 h) of repeated (2.0 g/kg, once daily for 7 days) ethanol administration. Additionally, the effects of VU-29 on expression of mGlu5 and mGlu2 receptor proteins in the hippocampus, prefrontal cortex, and striatum were determined 48 h after ethanol withdrawal. Our results indicated that VU-29, given before acute ethanol administration, prevented the ethanol-induced impairments in spatial memory retrieval. Furthermore, VU-29 given before the testing session on the first day of abstinence facilitated NOR performance in ethanol-withdrawn rats at 4- and 24-h delay after administration. Our ELISA results show that VU-29 normalized ethanol withdrawal induced increase in expression of mGlu5 receptor protein in the hippocampus, prefrontal cortex, and striatum, as well as expression of mGlu2 receptor protein in the hippocampus.
2.Cardiopulmonary effects of combined xylazine-guaiphenesin-ketamine infusion and extradural (inter-coccygeal lidocaine) anaesthesia in calves.
Picavet MT;Gasthuys FM;Laevens HH;Watts SA Vet Anaesth Analg. 2004 Jan;31(1):11-9.
OBJECTIVE: ;To investigate the cardiopulmonary effects of a xylazine-guaiphenesin-ketamine infusion combined with inter-coccygeal extradural (lidocaine) anaesthesia in calves.;STUDY DESIGN: ;Prospective study.;ANIMALS: ;Five Holstein Friesian calves (one steer, four heifers) aged 6 weeks weighing 65.2 +/- 2.7 kg.;MATERIALS AND METHODS: ;Calves were anaesthetized with isoflurane in oxygen for instrumentation. At least 12 hours later, xylazine (0.2 mg kg(-1) i.m.) was given. After 15 minutes, an infusion of xylazine hydrochloride (0.1 mg mL(-1)), guaiphenesin (50 mg mL(-1)) and ketamine (1 mg mL(-1)) (X-G-K) was infused at a rate of 1.1 mL kg(-1) hour-1 i.v. Oxygen (4 L minute(-1)) was delivered by nasotracheal tube 30 minutes later. Inter-coccygeal (Co1-Co2) extradural anaesthesia (lidocaine 2%, 0.18 mL kg(-1)) was administered 30 minutes later. Cardiopulmonary variables were obtained in the unsedated standing calves 10 minutes after xylazine, 15 and 30 minutes after X-G-K without O2, 15 and 30 minutes after X-G-K with O2 and 5, 15, 30, 45 and 60 minutes after extradural anaesthesia. Data were analysed using a repeated measurement analysis of variance including an autoregressive covariance structure of order 1 (correlations at different time intervals).
3.[Cardiovascular effects of a single dose of propofol in coronary patients with good ventricular function].
Pensado A;Molins N;Alvarez J Rev Esp Anestesiol Reanim. 1994 May-Jun;41(3):147-51.
OBJECTIVES: ;To determine the cardiovascular effects of a single dose of propofol in coronary patients with good ventricular function.;PATIENTS AND METHODS: ;Propofol 2 mg/kg-1 was administered to twenty coronary patients during dissection of the internal mammary artery in myocardial revascularization surgery. Heart rate (HR), systolic and diastolic systemic and pulmonary arterial pressure (SAP, DAP, SPAP and DPAP), central venous pressure, pulmonary capillary wedge pressure, cardiac output (CO), right ventricular ejection fraction, systemic and pulmonary vascular resistances (SVR and PVR), right and left ventricular stroke work index (RVSWI and LVSWI), rate-pressure product (RPP) and pressure-rate quotient (PRQ) were recorded prior to (baseline) and at 1, 3, 5, 10, 15, 20 and 30 min after administration of the drug.;RESULTS: ;One minute after administration of the drug there was a maximum decrease in SAP (-26%), DAP (-17%), SVR (-22%), RVSWI (-23%), RPP (-24%) and PRQ (-22%) (p < 0.001 in all cases) and this continued to be significant throughout the study for SAP, DAP and RPP, and for SVR, RVSWI and PRQ at times 15, 3 and 10, respectively. There were no significant changes in HR, CO, ventricular filling pressures and the remaining variables during the study.
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CAS 890764-36-0 VU 29

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