Improvements in the Pharmacological Profile of Diazepam by KRM-II-81, an Imidazodiazepine Positive Allosteric Modulator of 2/3-Containing GABAA Receptors: Preclinical Data Predict Enhanced Efficacy for Epilepsy, Chronic Pain, Anxiety, and Depression
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Jodi L. Smith | J. Witkin | J. Fisher | M. James | L. Golani | D. Knutson | J. Siemian | R. Černe | Cook | Justin N Siemian
[1] Jodi L. Smith,et al. The Positive Allosteric Modulator of α2/3-Containing GABAA Receptors, KRM-II-81, Is Active in Pharmaco-Resistant Models of Epilepsy and Reduces Hyperexcitability after Traumatic Brain Injury , 2019, The Journal of Pharmacology and Experimental Therapeutics.
[2] Jodi L. Smith,et al. The value of human epileptic tissue in the characterization and development of novel antiepileptic drugs: The example of CERC-611 and KRM-II-81 , 2019, Brain Research.
[3] M. Hall,et al. The Opioid Crisis and the Future of Addiction and Pain Therapeutics , 2019, The Journal of Pharmacology and Experimental Therapeutics.
[4] Donal N. Gorman,et al. Analgesic potential of PF-06372865, an α2/α3/α5 subtype-selective GABAA partial agonist, in humans. , 2019, British journal of anaesthesia.
[5] P. Davis,et al. The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats , 2019, Pharmacology Biochemistry and Behavior.
[6] R. M. Owen,et al. Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865). , 2019, Journal of medicinal chemistry.
[7] D. Buhl,et al. Pronounced antiepileptic activity of the subtype‐selective GABAA‐positive allosteric modulator PF‐06372865 in the GAERS absence epilepsy model , 2019, CNS neuroscience & therapeutics.
[8] K. Gee,et al. Positive allosteric modulators of nonbenzodiazepine &ggr;-aminobutyric acidA receptor subtypes for the treatment of chronic pain , 2018, Pain.
[9] D. Airey,et al. Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: Improved bioavailability enhances anticonvulsant efficacy , 2018, Neuropharmacology.
[10] G. Dawson,et al. Evidence That Sedative Effects of Benzodiazepines Involve Unexpected GABAA Receptor Subtypes: Quantitative Observation Studies in Rhesus Monkeys , 2018, The Journal of Pharmacology and Experimental Therapeutics.
[11] Hoon-Chul Kang,et al. Adverse Events During Perampanel Adjunctive Therapy in Intractable Epilepsy , 2018, Journal of clinical neurology.
[12] J. Fisher,et al. An antidepressant-related pharmacological signature for positive allosteric modulators of α2/3-containing GABAA receptors , 2018, Pharmacology Biochemistry and Behavior.
[13] Donal N. Gorman,et al. Pharmacology in translation: the preclinical and early clinical profile of the novel α2/3 functionally selective GABAA receptor positive allosteric modulator PF‐06372865 , 2018, British journal of pharmacology.
[14] L. Arnold,et al. Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors , 2017, Pharmacology Biochemistry and Behavior.
[15] R. Chou,et al. Systemic Pharmacologic Therapies for Low Back Pain: A Systematic Review for an American College of Physicians Clinical Practice Guideline , 2017, Annals of Internal Medicine.
[16] J. Fisher,et al. Antinociceptive Effects of a Novel α2/α3-Subtype Selective GABAA Receptor Positive Allosteric Modulator. , 2017, ACS chemical neuroscience.
[17] C. Halldin,et al. GABAA receptor occupancy by subtype selective GABAAα2,3 modulators: PET studies in humans , 2016, Psychopharmacology.
[18] J. Witkin,et al. Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy. , 2016, Journal of medicinal chemistry.
[19] P. Muglia,et al. NS11821, a partial subtype-selective GABAA agonist, elicits selective effects on the central nervous system in randomized controlled trial with healthy subjects , 2016, Journal of psychopharmacology.
[20] William T. Ralvenius,et al. Analgesia and unwanted benzodiazepine effects in point-mutated mice expressing only one benzodiazepine-sensitive GABAA receptor subtype , 2015, Nature Communications.
[21] Y. Daali,et al. GABAergic modulation in central sensitization in humans: a randomized placebo-controlled pharmacokinetic–pharmacodynamic study comparing clobazam with clonazepam in healthy volunteers , 2015, Pain.
[22] P. Maruff,et al. The central nervous system effects of the partial GABA-Aα2,3 -selective receptor modulator AZD7325 in comparison with lorazepam in healthy males. , 2014, British journal of clinical pharmacology.
[23] K. Gee,et al. Limited central side effects of a β-subunit subtype-selective GABAA receptor allosteric modulator , 2014, Journal of psychopharmacology.
[24] J. Barrow,et al. Classics in chemical neuroscience: diazepam (valium). , 2014, ACS chemical neuroscience.
[25] U. Rudolph,et al. GABAA receptor subtypes: Therapeutic potential in Down syndrome, affective disorders, schizophrenia, and autism. , 2014, Annual review of pharmacology and toxicology.
[26] P. Skolnick. Anxioselective anxiolytics: on a quest for the Holy Grail. , 2012, Trends in pharmacological sciences.
[27] J. Cook,et al. The role of &agr;1 and &agr;5 subunit-containing GABAA receptors in motor impairment induced by benzodiazepines in rats , 2012, Behavioural pharmacology.
[28] R. Schoemaker,et al. The effects of TPA023, a GABAAα2,3 subtype-selective partial agonist, on essential tremor in comparison to alcohol , 2012, Journal of psychopharmacology.
[29] J. Conry,et al. Randomized, phase III study results of clobazam in Lennox-Gastaut syndrome , 2011, Neurology.
[30] F. Knoflach,et al. Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypes , 2011, Nature Reviews Drug Discovery.
[31] J. Atack,et al. GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics. , 2011, Current topics in medicinal chemistry.
[32] David Taylor,et al. Efficacy of drug treatments for generalised anxiety disorder: systematic review and meta-analysis , 2011, BMJ : British Medical Journal.
[33] P. Czobor,et al. A Multicenter, Placebo‐Controlled, Double‐Blind, Randomized Study of Efficacy and Safety of Ocinaplon (DOV 273,547) in Generalized Anxiety Disorder , 2010, CNS neuroscience & therapeutics.
[34] J. Belluzzi,et al. Limiting Activity at β1-Subunit-Containing GABAA Receptor Subtypes Reduces Ataxia , 2010, Journal of Pharmacology and Experimental Therapeutics.
[35] Kelly R. Tan,et al. Neural bases for addictive properties of benzodiazepines , 2010, Nature.
[36] G. Dawson,et al. Reducing Abuse Liability of GABAA/Benzodiazepine Ligands via Selective Partial Agonist Efficacy at α1 and α2/3 Subtypes , 2010, Journal of Pharmacology and Experimental Therapeutics.
[37] J. Baron,et al. Benzodiazepine Binding Site Occupancy by the Novel GABAA Receptor Subtype-Selective Drug 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in Rats, Primates, and Humans , 2010, Journal of Pharmacology and Experimental Therapeutics.
[38] J. Atack. GABAA receptor alpha2/alpha3 subtype-selective modulators as potential nonsedating anxiolytics. , 2010, Current topics in behavioral neurosciences.
[39] N. Mirza,et al. Developing analgesics by enhancing spinal inhibition after injury: GABAA receptor subtypes as novel targets. , 2009, Trends in pharmacological sciences.
[40] B. Roth,et al. Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. , 2009, Journal of medicinal chemistry.
[41] H. Zeilhofer,et al. Genuine Antihyperalgesia by Systemic Diazepam Revealed by Experiments in Gaba a Receptor Point-mutated Mice , 2008 .
[42] R. Olsen,et al. GABAA receptors: Subtypes provide diversity of function and pharmacology , 2009, Neuropharmacology.
[43] J. Atack. Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023. , 2009, Advances in pharmacology.
[44] S. C. Licata,et al. Contribution of α1 subunit-containing γ-aminobutyric acidA (GABAA) receptors to motor-impairing effects of benzodiazepines in squirrel monkeys , 2009, Psychopharmacology.
[45] Andrea Tone,et al. The Age of Anxiety: A History of America's Turbulent Affair with Tranquilizers , 2008 .
[46] W. Sieghart,et al. Are GABAA Receptors Containing α5 Subunits Contributing to the Sedative Properties of Benzodiazepine Site Agonists? , 2008, Neuropsychopharmacology.
[47] J. Gerven,et al. Pharmacodynamic and pharmacokinetic effects of TPA023, a GABAA α2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers , 2007 .
[48] N Collinson,et al. An Inverse Agonist Selective for α5 Subunit-Containing GABAA Receptors Enhances Cognition , 2006, Journal of Pharmacology and Experimental Therapeutics.
[49] G. Dawson,et al. TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates , 2006, Journal of Pharmacology and Experimental Therapeutics.
[50] G. Dawson,et al. 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. , 2005, Journal of medicinal chemistry.
[51] G. Dawson,et al. Evidence for a Significant Role of α3-Containing GABAA Receptors in Mediating the Anxiolytic Effects of Benzodiazepines , 2005, The Journal of Neuroscience.
[52] P. Czobor,et al. Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator. , 2005, Proceedings of the National Academy of Sciences of the United States of America.
[53] K. Wafford. GABAA receptor subtypes: any clues to the mechanism of benzodiazepine dependence? , 2005, Current opinion in pharmacology.
[54] W. Haefely. Pharmacology of the benzodiazepine receptor , 2004, European archives of psychiatry and neurological sciences.
[55] C. Allgulander,et al. Efficacy of usual antidepressant dosing regimens of fluoxetine in panic disorder , 2001, British Journal of Psychiatry.
[56] I Tobler,et al. Diazepam-induced changes in sleep: role of the alpha 1 GABA(A) receptor subtype. , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[57] T. Rülicke,et al. Molecular and neuronal substrate for the selective attenuation of anxiety. , 2000, Science.
[58] R. Mckernan,et al. Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype , 2000, Nature Neuroscience.
[59] S. Woods,et al. Changes of benzodiazepine receptors during chronic benzodiazepine administration in humans. , 1999, European journal of pharmacology.
[60] J. Benson,et al. Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. , 1999, Nature.
[61] W. Hevers,et al. The diversity of GABAA receptors. Pharmacological and electrophysiological properties of GABAA channel subtypes. , 1998, Molecular neurobiology.
[62] M. Bousoño,et al. SSRI-induced sexual dysfunction: fluoxetine, paroxetine, sertraline, and fluvoxamine in a prospective, multicenter, and descriptive clinical study of 344 patients. , 1997, Journal of sex & marital therapy.
[63] S. Koslow,et al. Onset of antidepressant activity: Reexamining the structure of depression and multiple actions of drugs , 1996, Depression and anxiety.
[64] N. Ryan,et al. Fluoxetine for childhood anxiety disorders. , 1994, Journal of the American Academy of Child and Adolescent Psychiatry.
[65] B. Denis,et al. [Hepatitis induced by alpidem (Ananxyl). Four cases, one of them fatal]. , 1994, Gastroenterologie clinique et biologique.
[66] J. Fritschy,et al. GABAA-receptor subtypes differing in alpha-subunit composition display unique pharmacological properties. , 1992, Advances in biochemical psychopharmacology.
[67] G. Mawer,et al. Respiratory and sedative effects of clobazam and clonazepam in volunteers. , 1990, British journal of clinical pharmacology.
[68] P. Morselli,et al. Clinical studies with the new anxiolytic alpidem in anxious patients: An overview of the European experiences , 1988, Pharmacology Biochemistry and Behavior.
[69] B. Maletzky. Anxiolytic Efficacy of Alprazolam Compared to Diazepam and Placebo , 1980, The Journal of international medical research.
[70] G. Aden,et al. Alprazolam compared to diazepam and placebo in the treatment of anxiety. , 1980, The Journal of clinical psychiatry.
[71] B. Beer,et al. Resolution of two biochemically and pharmacologically distinct benzodiazepine receptors , 1979, Pharmacology Biochemistry and Behavior.
[72] S. Paul,et al. Labelling of benzodiazepine receptors in vivo , 1978, Nature.
[73] C. Braestrup,et al. Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding. , 1977, Proceedings of the National Academy of Sciences of the United States of America.
[74] G. Fischbach,et al. Chlordiazepoxide selectively augments GABA action in spinal cord cell cultures , 1977, Nature.
[75] H. Parry,et al. National patterns of psychotherapeutic drug use. , 1973, Archives of general psychiatry.
[76] J. Overall,et al. DIAZEPAM IN NEWLY ADMITTED SCHIZOPHRENICS. , 1963, Diseases of the nervous system.
[77] G. A. Heise,et al. The psychosedative properties of methaminodiazepoxide. , 1960, The Journal of pharmacology and experimental therapeutics.