Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Roman Furtmüller"'
Autor:
Lalit K. Golani, Donna M. Platt, Daniela Rüedi-Bettschen, Chitra Edwanker, Shenming Huang, Michael M. Poe, Roman Furtmüller, Werner Sieghart, James M. Cook, James K. Rowlett
Publikováno v:
Frontiers in Pharmacology, Vol 12 (2021)
In order to develop improved anxiolytic drugs, 8-substituted analogs of triazolam were synthesized in an effort to discover compounds with selectivity for α2/α3 subunit-containing GABAA subtypes. Two compounds in this series, XLi-JY-DMH (6-(2-chlor
Externí odkaz:
https://doaj.org/article/a95252a7ff224cdca9d223b58e02c490
Autor:
Lalit K, Golani, Donna M, Platt, Daniela, Rüedi-Bettschen, Chitra, Edwanker, Shenming, Huang, Michael M, Poe, Roman, Furtmüller, Werner, Sieghart, James M, Cook, James K, Rowlett
Publikováno v:
Frontiers in Pharmacology
In order to develop improved anxiolytic drugs, 8-substituted analogs of triazolam were synthesized in an effort to discover compounds with selectivity for α2/α3 subunit-containing GABAA subtypes. Two compounds in this series, XLi-JY-DMH (6-(2-chlor
Autor:
Terry Clayton, James M. Cook, Danni L. Harris, Peyman Sahbaie, Timothy M. DeLorey, Robert F. Halliwell, Werner Sieghart, Sigismund Huck, Roman Furtmüller
Publikováno v:
Journal of Medicinal Chemistry. 51:3788-3803
Ligands that bind to the benzodiazepine binding site on the GABA A receptor can attenuate or potentiate cognition. To investigate this property, the chemical determinants favoring selective binding or selective activation of the alpha5beta2gamma2 and
Autor:
Lars Richter, Gerhard F. Ecker, Michael W. Parker, Catherine C. Kaczorowski, J. L. Chen, Margot Ernst, Brett A. Cromer, Werner Sieghart, F. J. Helmstetter, H.-L. Ng, Craig J. Morton, Roman Furtmüller, James M. Cook, Terrill Scott Clayton
Publikováno v:
Current Medicinal Chemistry. 14:2755-2775
A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of
Autor:
Terry Clayton, Werner Sieghart, James M. Cook, Roman Furtmüller, Nenad D. Ugrešić, Miroslav M. Savić, Sigismund Huck, Dubravko Bokonjić, Shengming Huang, Dragan I. Obradović
Publikováno v:
Neuropsychopharmacology
Classical benzodiazepines (BZs) exert anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsive, and amnesic effects through potentiation of neurotransmission at GABA(A) receptors containing alpha(1), alpha(2), alpha(3) or alpha(5) subunits. Ge
Autor:
Roman Furtmüller, Ahmed El Hadri, Werner Sieghart, Roland Baur, Erwin Sigel, Robert H. Dodd, Urs Thomet, Ahmed Abouabdellah
Publikováno v:
Journal of Medicinal Chemistry. 45:2824-2831
1,4-Addition of benzylamine to 2(5H)-furanone followed by dialkylation of the 3-position with allylbromide gave (+/-)-4-benzyl-3,3-diallyl-2(3H)-furanone (8), which served as the intermediate for the synthesis of various N-substituted 4-amino-3,3-dip
Autor:
M. G. Schlag, Werner Sieghart, Rudolf Hopf, Sigismund Huck, Michael L. Berger, Heinz Redl, Roman Furtmüller
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 301:168-173
Application of 4-(aminomethyl)cyclohexanecarboxylic acid (tranexamic acid; TAMCA) to the central nervous system (CNS) has been shown to result in hyperexcitability and convulsions. However, the mechanisms underlying this action are unknown. In the pr
Autor:
Frantisek Jursky, Werner Sieghart, Roman Furtmüller, Erwin Sigel, Urs Thomet, Robert H. Dodd, Rodolphe Razet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2579-2583
Analogues of bicuculline devoid of the benzo ring fused to the lactone moiety were prepared by reacting 2-( tert -butyldimethylsiloxy)furans with 3,4-dihydroisoquinolinium salts. Some of these compounds (e.g., ROD185, 8 ) acted as modulators of the G
Autor:
Rodolphe Razet, Roman Furtmüller, Roland Baur, Urs Thomet, Robert H. Dodd, Werner Sieghart, Erwin Sigel
Publikováno v:
British Journal of Pharmacology. 131:843-850
(+)-ROD188 was synthesized in the search for novel ligands of the GABA binding site. It shares some structural similarity with bicuculline. (+)-ROD188 failed to displace [3H]-muscimol in binding studies and failed to induce channel opening in recombi
Autor:
Patrice Venault, Jean-François Rousseau, Robert H. Dodd, Erwin Sigel, Georges Chapouthier, Roman Furtmüller, Werner Sieghart, Mireille Le Hyaric-Almeida, Urs Thomet
Publikováno v:
Neuroscience Letters. 269:63-66
Rat recombinant alpha1beta2gamma2 gamma-aminobutyric acid type A (GABAA) receptors were functionally expressed in Xenopus laevis oocytes and analyzed for the action of EDPC (Ethyl 3-(1,3-dithian-2-yl)-1H-pyrrolo[2,3-c]pyridine-5-carboxylate) using el