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Determination of tautomeric preference of fenobam in solution by high-resolution NMR spectroscopy.
Sha X, Chen S, Zheng X, Ye X, Zhang H, Huang S. Sha X, et al. Magn Reson Chem. 2021 Jun;59(6):641-647. doi: 10.1002/mrc.5127. Epub 2021 Jan 14. Magn Reson Chem. 2021. PMID: 33368586
In this work, tautomeric preference of fenobam in solution was investigated by homonuclear and heteronuclear solution nuclear magnetic resonance (NMR) spectroscopy. (1) H-(1) H nuclear Overhauser effect spectroscopy (NOESY) spectrum revealed that fenobam in liquid s …
In this work, tautomeric preference of fenobam in solution was investigated by homonuclear and heteronuclear solution nuclear magneti …
Novel non-benzodiazepine anxiolytics.
Goldberg ME, Salama AI, Patel JB, Malick JB. Goldberg ME, et al. Neuropharmacology. 1983 Dec;22(12B):1499-504. doi: 10.1016/0028-3908(83)90118-1. Neuropharmacology. 1983. PMID: 6142427 Review.
These include tracazolate, zopiclone, CL218,872, CGS9896, buspirone, MK-801 and fenobam. A comparison of anticonflict effects and propensity to cause sedation and potentiate the actions of ethanol is given as well as their effects upon the binding of [3H]flunitrazepam in v …
These include tracazolate, zopiclone, CL218,872, CGS9896, buspirone, MK-801 and fenobam. A comparison of anticonflict effects and pro …
Clinical investigations of compounds targeting metabotropic glutamate receptors.
Witkin JM, Pandey KP, Smith JL. Witkin JM, et al. Pharmacol Biochem Behav. 2022 Sep;219:173446. doi: 10.1016/j.pbb.2022.173446. Epub 2022 Aug 17. Pharmacol Biochem Behav. 2022. PMID: 35987339 Review.
Efficacy with mGlu5R antagonists has been reported in trials with patients with gastroesophageal reflux disease; data from patients with Parkinson's disease or Fragile X syndrome have not been as robust as hoped. Fenobam was approved for use as an anxiolytic prior to its r …
Efficacy with mGlu5R antagonists has been reported in trials with patients with gastroesophageal reflux disease; data from patients with Par …
Fenobam promoted the neuroprotective effect of PEP-1-FK506BP following oxidative stress by increasing its transduction efficiency.
Ahn EH, Kim DW, Shin MJ, Jo HS, Eom SA, Kim DS, Park EY, Park JH, Cho SW, Park J, Eum WS, Son O, Hwang HS, Choi SY. Ahn EH, et al. BMB Rep. 2013 Nov;46(11):561-6. doi: 10.5483/bmbrep.2013.46.11.080. BMB Rep. 2013. PMID: 24152913 Free PMC article.
Fenobam strongly enhanced the protective effect of PEP-1-FK506BP against H2O2-induced toxicity and DNA fragmentation in C6 cells. ...Interestingly, our results showed that fenobam significantly increased the transduction of PEP-1-FK506BP into both C6 cells and the h …
Fenobam strongly enhanced the protective effect of PEP-1-FK506BP against H2O2-induced toxicity and DNA fragmentation in C6 cells. ... …
The metabotropic glutamate receptor 5 negative allosteric modulator fenobam: pharmacokinetics, side effects, and analgesic effects in healthy human subjects.
Cavallone LF, Montana MC, Frey K, Kallogjeri D, Wages JM, Rodebaugh TL, Doshi T, Kharasch ED, Gereau RW 4th. Cavallone LF, et al. Pain. 2020 Jan;161(1):135-146. doi: 10.1097/j.pain.0000000000001695. Pain. 2020. PMID: 31568235 Free PMC article. Clinical Trial.
Analgesic effects of fenobam in humans have not been reported. The purpose of this investigation was to evaluate fenobam pharmacokinetics and analgesic effects in humans. ...Fenobam reduced sensitization vs placebo at a single timepoint (peak plasma concentra …
Analgesic effects of fenobam in humans have not been reported. The purpose of this investigation was to evaluate fenobam pharm …
Inhibiting metabotropic glutamate receptor 5 after stroke restores brain function and connectivity.
Hakon J, Quattromani MJ, Sjölund C, Talhada D, Kim B, Moyanova S, Mastroiacovo F, Di Menna L, Olsson R, Englund E, Nicoletti F, Ruscher K, Bauer AQ, Wieloch T. Hakon J, et al. Brain. 2024 Jan 4;147(1):186-200. doi: 10.1093/brain/awad293. Brain. 2024. PMID: 37656990 Free PMC article.
Using multiple behavioural tests, we observed that treatment with negative allosteric modulators (NAMs) of mGluR5 (MTEP, fenobam and AFQ056) for 12 days, starting 2 or 10 days after stroke, restored lost sensorimotor functions, without diminishing infarct size. ...
Using multiple behavioural tests, we observed that treatment with negative allosteric modulators (NAMs) of mGluR5 (MTEP, fenobam and …
The mGluR5 antagonist fenobam induces analgesic conditioned place preference in mice with spared nerve injury.
Lax NC, George DC, Ignatz C, Kolber BJ. Lax NC, et al. PLoS One. 2014 Jul 25;9(7):e103524. doi: 10.1371/journal.pone.0103524. eCollection 2014. PLoS One. 2014. PMID: 25061818 Free PMC article.
This study was done to look at the possible rewarding properties of the mGluR5 antagonist, fenobam, in a cognitive assay. Analgesic conditioned place preference (aCPP) was used to examine the effects of fenobam (30 mg/kg) and the prototypical mGluR5 antagonist, MPEP …
This study was done to look at the possible rewarding properties of the mGluR5 antagonist, fenobam, in a cognitive assay. Analgesic c …
The pro-psychotic metabotropic glutamate receptor compounds fenobam and AZD9272 share binding sites with monoamine oxidase-B inhibitors in humans.
Varnäs K, Cselényi Z, Arakawa R, Nag S, Stepanov V, Moein MM, Johnström P, Kingston L, Elmore CS, Halldin C, Farde L. Varnäs K, et al. Neuropharmacology. 2020 Jan 1;162:107809. doi: 10.1016/j.neuropharm.2019.107809. Epub 2019 Oct 4. Neuropharmacology. 2020. PMID: 31589885 Free article.
The metabotropic glutamate receptor 5 (mGluR5) ligands fenobam and AZD9272 have been reported to induce psychosis-like adverse events and to bind at unknown, non-GluR5-related, sites. ...In PET studies of NHP brain administration of the MAO-B ligand L-deprenyl inhibited bi …
The metabotropic glutamate receptor 5 (mGluR5) ligands fenobam and AZD9272 have been reported to induce psychosis-like adverse events …
Metabotropic glutamate receptor 5 antagonism with fenobam: examination of analgesic tolerance and side effect profile in mice.
Montana MC, Conrardy BA, Cavallone LF, Kolber BJ, Rao LK, Greco SC, Gereau RW 4th. Montana MC, et al. Anesthesiology. 2011 Dec;115(6):1239-50. doi: 10.1097/ALN.0b013e318238c051. Anesthesiology. 2011. PMID: 22037639 Free PMC article.
METHODS: Mouse models of pain, locomotor behavior, and coordination were used. Fenobam or vehicle (n = 8 or 11 per group) was administered for 14 days, and analgesic tolerance to fenobam was assessed using the formalin test. ...Fenobam represents a promising …
METHODS: Mouse models of pain, locomotor behavior, and coordination were used. Fenobam or vehicle (n = 8 or 11 per group) was adminis …
Fenobam sulfate inhibits cocaine-taking and cocaine-seeking behavior in rats: implications for addiction treatment in humans.
Keck TM, Yang HJ, Bi GH, Huang Y, Zhang HY, Srivastava R, Gardner EL, Newman AH, Xi ZX. Keck TM, et al. Psychopharmacology (Berl). 2013 Sep;229(2):253-65. doi: 10.1007/s00213-013-3106-9. Epub 2013 Apr 25. Psychopharmacology (Berl). 2013. PMID: 23615919 Free PMC article.
RESULTS: In rats, fenobam sulfate had superior pharmacokinetics compared to the free base, with improved maximal plasma concentration (C max) and longer half life. ...Fenobam sulfate also inhibited p.o. sucrose self-administration and sucrose-induced reinstatement o …
RESULTS: In rats, fenobam sulfate had superior pharmacokinetics compared to the free base, with improved maximal plasma concentration …
69 results