| References |
Top |
| REF 1 |
Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
|
| REF 2 |
Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
|
| REF 3 |
Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
|
| REF 4 |
Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
|
| REF 5 |
URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6963).
|
| REF 6 |
FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074569.
|
| REF 7 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008928)
|
| REF 8 |
2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
|
| REF 9 |
URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2804).
|
| REF 10 |
Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
|
| REF 11 |
FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080671.
|
| REF 12 |
Adjunctive topiramate enhances the risk of hypothermia associated with valproic acid therapy. J Clin Pharm Ther. 2008 Oct;33(5):513-9.
|
| REF 13 |
URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4346).
|
| REF 14 |
Abecarnil enhances GABA-induced currents in acutely isolated cerebellar Purkinje cells. Neuropharmacology. 1995 Feb;34(2):157-63.
|
| REF 15 |
The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
|
| REF 16 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030421)
|
| REF 17 |
Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
|
| REF 18 |
Emerging drugs to treat Crohn's disease. Expert Opin Emerg Drugs. 2007 Mar;12(1):49-59.
|
| REF 19 |
URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8480).
|
| REF 20 |
Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
|
| REF 21 |
ClinicalTrials.gov (NCT00940186) Clinical Pharmacokinetics Study on Pikamilone. U.S. National Institutes of Health.
|
| REF 22 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005875)
|
| REF 23 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000082)
|
| REF 24 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005436)
|
| REF 25 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001194)
|
| REF 26 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021837)
|
| REF 27 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000696)
|
| REF 28 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001470)
|
| REF 29 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004007)
|
| REF 30 |
Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes. J Med Chem. 2006 Jul 27;49(15):4595-605.
|
| REF 31 |
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18.
|
| REF 32 |
Hyperekplexia in neonates. Postgrad Med J. 2001 Sep;77(911):570-2.
|
| REF 33 |
DP-VPA D-Pharm. Curr Opin Investig Drugs. 2002 Jun;3(6):921-3.
|
| REF 34 |
DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
|
| REF 35 |
Anticonvulsant drugs: mechanisms of action. Adv Neurol. 1986;44:713-36.
|
| REF 36 |
Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Int J Antimicrob Agents. 2003 Sep;22(3):318-31.
|
| REF 37 |
3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
|
| REF 38 |
Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
|
| REF 39 |
Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9.
|
| REF 40 |
50 years of hurdles and hope in anxiolytic drug discovery. Nat Rev Drug Discov. 2013 Sep;12(9):667-87.
|
| REF 41 |
Clobazam, oxcarbazepine, tiagabine, topiramate, and other new antiepileptic drugs. Epilepsia. 1995;36 Suppl 2:S105-14.
|
| REF 42 |
US patent application no. US20040102438 A1.
|
| REF 43 |
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. J Med Chem. 1999 Apr 8;42(7):1123-44.
|
| REF 44 |
Capreomycin Binds across the Ribosomal Subunit Interface Using tlyA-Encoded 2 O-Methylations in 16S and 23S rRNAs. Molecular Cell Volume 23, Issue 2, 21 July 2006, Pages 173-182.
|
| REF 45 |
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.
|
| REF 46 |
Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. J Med Chem. 2006 Mar 23;49(6):1855-66.
|
| REF 47 |
(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics. J Med Chem. 1988 Jun;31(6):1220-6.
|
| REF 48 |
U-90042, a sedative/hypnotic compound that interacts differentially with the GABAA receptor subtypes. J Pharmacol Exp Ther. 1995 Nov;275(2):761-7.
|
| REF 49 |
Regulation of neuronal and recombinant GABA(A) receptor ion channels by xenovulene A, a natural product isolated from Acremonium strictum. J Pharmacol Exp Ther. 1997 Aug;282(2):513-20.
|
| REF 50 |
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships. J Med Chem. 2008 Jul 10;51(13):3825-40.
|
| REF 51 |
( )-2-amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist. Bioorg. Med. Chem. Lett. 1(5):247-248 (1991).
|
| REF 52 |
gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
|
| REF 53 |
Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists. J Med Chem. 1987 Apr;30(4):750-3.
|
| REF 54 |
Benzodiazepine receptor binding activity of 6,9-disubstituted purines. J Med Chem. 1989 May;32(5):1020-4.
|
| REF 55 |
3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam. J Med Chem. 1985 Jun;28(6):824-8.
|
| REF 56 |
Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. J Med Chem. 1992 Jun 12;35(12):2214-20.
|
| REF 57 |
Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):402-4.
|
| REF 58 |
Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant ... J Med Chem. 1994 Jan 21;37(2):275-86.
|
| REF 59 |
Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ... J Med Chem. 1988 Jan;31(1):1-3.
|
| REF 60 |
Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach. J Med Chem. 1992 Oct 30;35(22):4001-10.
|
| REF 61 |
Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions. J Med Chem. 1986 Feb;29(2):224-9.
|
| REF 62 |
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological p... J Med Chem. 1998 May 21;41(11):1846-54.
|
| REF 63 |
Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor. J Med Chem. 2002 Sep 12;45(19):4188-201.
|
| REF 64 |
Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor, Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997).
|
| REF 65 |
Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51.
|
| REF 66 |
Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. J Med Chem. 1996 Jul 19;39(15):2915-21.
|
| REF 67 |
Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64.
|
| REF 68 |
A study of 3-amino-N-hydroxypropanesulfonamide derivatives as potential GABAB agonists and their fragmentation to 3-aminopropanesulfinic acid, Bioorg. Med. Chem. Lett. 6(14):1709-1714 (1996).
|
| REF 69 |
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore mod... J Med Chem. 2006 Apr 20;49(8):2526-33.
|
| REF 70 |
Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. J Med Chem. 1988 Sep;31(9):1854-61.
|
| REF 71 |
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
|
| REF 72 |
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors. J Med Chem. 1982 Oct;25(10):1157-62.
|
| REF 73 |
Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site. J Med Chem. 1990 Sep;33(9):2343-57.
|
| REF 74 |
N-2 methylated quaternary derivatives of beta-carboline-3-carboxylates inhibit acetylcholinesterase in vitroO, Bioorg. Med. Chem. Lett. 3(12):2831-2836 (1993).
|
| REF 75 |
Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem. 1994 Dec 23;37(26):4576-80.
|
| REF 76 |
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of ga... J Med Chem. 2006 Jul 13;49(14):4442-6.
|
| REF 77 |
Synthesis of carbon-11-, fluorine-18-, and iodine-125-labeled GABAA-gated chloride ion channel blockers: substituted 5-tert-butyl-2-phenyl-1,3-dith... J Med Chem. 1995 Jul 7;38(14):2663-71.
|
| REF 78 |
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol. J Med Chem. 1985 Nov;28(11):1612-7.
|
| REF 79 |
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. J Med Chem. 2006 Feb 23;49(4):1388-96.
|
| REF 80 |
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. J Med Chem. 2005 Jan 27;48(2):427-39.
|
| REF 81 |
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology. J Med Chem. 2000 Dec 28;43(26):4930-3.
|
| REF 82 |
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. J Med Chem. 2007 Apr 19;50(8):1988-92.
|
| REF 83 |
6-Bromo-3 nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites, Bioorg. Med. Chem. Lett. 7(3):373-378 (1997).
|
| REF 84 |
6,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties, Bioorg. Med. Chem. Lett. 5(22):2717-2720 (1995).
|
| REF 85 |
Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands. J Med Chem. 1987 Mar;30(3):456-8.
|
| REF 86 |
Aryl diazo compounds and diazonium salts as potential irreversible probes of the gamma-aminobutyric acid receptor. J Med Chem. 1987 Dec;30(12):2222-7.
|
| REF 87 |
beta-Carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of beta-carboline-3-carboxylic a... J Med Chem. 1983 Apr;26(4):499-503.
|
| REF 88 |
Partial structures of the fungal toxin aflatrem, methyl-substituted 6,8-dioxabicyclo[3.2.1]octan-2-ones have anticonvulsant activity, Bioorg. Med. Chem. Lett. 5(3):265-270 (1995).
|
| REF 89 |
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
|
| REF 90 |
Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high af... J Med Chem. 1995 Jan 6;38(1):189-98.
|
| REF 91 |
GABA receptors inhibited by benzodiazepines mediate fast inhibitory transmission in the central amygdala. J Neurosci. 1999 Nov 15;19(22):9698-704.
|
| REF 92 |
Isosteric replacement of the indole nucleus by benzothiophene in a series of pyrido[2,3-b]indoles with potential anxiolytic activity, Bioorg. Med. Chem. Lett. 5(22):2589-2592 (1995).
|
| REF 93 |
Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. J Med Chem. 1991 Jan;34(1):281-90.
|
| REF 94 |
1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. J Med Chem. 1987 Oct;30(10):1737-42.
|
| REF 95 |
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor li... J Med Chem. 2004 Mar 25;47(7):1807-22.
|
| REF 96 |
THIP treatment of Huntington's disease. Neurology. 1983 May;33(5):637-9.
|
| REF 97 |
N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological acti... J Med Chem. 1998 Sep 24;41(20):3821-30.
|
| REF 98 |
Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-... J Med Chem. 2007 Apr 5;50(7):1627-34.
|
| REF 99 |
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular mo... J Med Chem. 2001 Jul 5;44(14):2286-97.
|
| REF 100 |
Orally active and potent inhibitors of gamma-aminobutyric acid uptake. J Med Chem. 1985 May;28(5):653-60.
|
| REF 101 |
Structure and molecular modeling of GABAA receptor antagonists. J Med Chem. 1992 May 29;35(11):1969-77.
|
| REF 102 |
Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. J Med Chem. 1989 Dec;32(12):2561-73.
|
| REF 103 |
Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in r... J Med Chem. 1985 May;28(5):683-5.
|
| REF 104 |
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem. 1988 Dec;31(12):2235-46.
|
| REF 105 |
Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepin... J Med Chem. 1993 Apr 16;36(8):1001-6.
|
| REF 106 |
The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
|
| REF 107 |
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment... Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4.
|
| REF 108 |
Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. J Med Chem. 1995 Jan 6;38(1):16-20.
|
| REF 109 |
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42.
|
| REF 110 |
Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. J Med Chem. 1994 Mar 18;37(6):758-68.
|
| REF 111 |
Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation. Bioorg Med Chem Lett. 2001 Feb 12;11(3):283-6.
|
| REF 112 |
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
|
| REF 113 |
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABA... J Med Chem. 1996 Apr 26;39(9):1928-34.
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