SGS742: the first GABAB receptor antagonist in clinical trials

Biochemical Pharmacology - Tập 68 - Trang 1479-1487 - 2004
Wolfgang Froestl1, Michela Gallagher2, Helen Jenkins3, Annette Madrid3, Thorsten Melcher3, Sam Teichman3, Cesare G. Mondadori4, Rodney Pearlman3
1Neuroscience Research, Novartis Pharma AG, WKL-136.5.25, CH-4002 Basel, Switzerland
2Department of Psychology, Johns Hopkins University, Baltimore, MD 21218, USA
3Saegis Pharmaceuticals, Inc., Half Moon Bay, CA 94019, USA
4Neuro3D SA, F-68086 Mulhouse, France

Tài liệu tham khảo

Bowery, 2002, International Union of Pharmacology XXXIII. Mammalian γ-aminobutyric acidB receptors: structure and function, Pharmacol Rev, 54, 247, 10.1124/pr.54.2.247 Froestl, 1995, Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists, J Med Chem, 38, 3313, 10.1021/jm00017a016 Chebib, 1997, Unsaturated phosphinic analogues of γ-aminobutyric acid as GABAC receptor antagonists, Eur J Pharmacol, 329, 223, 10.1016/S0014-2999(97)89183-2 Beaumont, 1978, Muscimol binding in rat brain: association with synaptic GABA receptors, Brain Res, 148, 153, 10.1016/0006-8993(78)90385-2 Olpe, 1993, The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro, Eur J Pharmacol, 233, 179, 10.1016/0014-2999(93)90048-M Olpe, 1994, Contribution of presynaptic GABA-B receptors to paired-pulse depression of GABA-responses in the hippocampus, Naunyn-Schmiedeberg's Arch Pharmacol, 349, 473, 10.1007/BF00169135 Bonanno, 1999, Selective block of rat and human neocortex GABAB receptors regulating somatostatin release by a GABAB antagonist endowed with cognition enhancing activity, Neuropharmacology, 38, 1789, 10.1016/S0028-3908(99)00084-2 Pittaluga, 2001, Potentiation of NMDA receptor function through somatostatin release: a possible mechanism for the cognition-enhancing activity of GABAB receptor antagonists, Neuropharmacology, 41, 301, 10.1016/S0028-3908(01)00066-1 Nyitrai, 2003, GABAB receptor antagonist CGP-36742 enhances somatostatin release in the rat hippocampus in vivo and in vitro, Eur J Pharmacol, 478, 111, 10.1016/j.ejphar.2003.08.006 Pratt, 1993, Repeated administration of desipramine and a GABAB receptor antagonist, CGP36742, discreetly up-regulates GABAB receptor binding sites in rat frontal cortex, Br J Pharmacol, 110, 724, 10.1111/j.1476-5381.1993.tb13872.x Nyitrai, 1999, Effect of CGP36742 on the extracellular level of neurotransmitter amino acids in the thalamus, Neurochem Int, 34, 391, 10.1016/S0197-0186(99)00042-X Olpe, 1993, Stimulation parameters determine role of GABAB receptors in long-term potentiation, Experientia, 49, 542, 10.1007/BF01955159 Mondadori, 1993, CGP36742: the first orally active GABAB blocker improves the cognitive performance of mice, rats, and Rhesus monkeys, Behav Neural Biol, 60, 62, 10.1016/0163-1047(93)90729-2 Mondadori, 1996, The GABAB receptor antagonist CGP36742 and the nootropic oxiracetam facilitate the formation of long-term memory, Behav Brain Res, 77, 223, 10.1016/0166-4328(95)00222-7 Carletti, 1993, The GABA-B antagonist CGP36742 enhances spatial learning performance and antagonises baclofen-induced amnesia in mice, Br J Pharmacol, 109, 74 Nakagawa, 1997, The GABAB receptor antagonist CGP36742 attenuates the baclofen- and scopolamine-induced deficit in Morris water maze task in rats, Brain Res, 766, 101, 10.1016/S0006-8993(97)00529-5 Mondadori, 1996, CGP36742, an orally active GABAB receptor antagonist, facilitates memory in a social recognition test in rats, Behav Brain Res, 77, 227, 10.1016/0166-4328(95)00226-X Getova, 1997, Effects of GABAB receptor antagonists on learning and memory retention in a rat model of absence epilepsy, Eur J Pharmacol, 320, 9, 10.1016/S0014-2999(96)00877-1 Nakagawa, 1999, The GABAB receptor antagonist CGP36742 improves learned helplessness in rats, Eur J Pharmacol, 381, 1, 10.1016/S0014-2999(99)00567-1 Heese, 2000, GABAB receptor antagonists elevate both mRNA and protein levels of the neurotrophins nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) but not neurotophin-3 (NT-3) in brain and spinal cord of rats, Neuropharmacology, 39, 449, 10.1016/S0028-3908(99)00166-5 Saegis Pharmaceuticals, Inc. SGS742: Investigator's Brochure, Version 5, updated Feb. 11, 2004. Tomlinson J, Cummins H, Wendt J, Margolin D, Pahl J, Jenkins H, Pearlman R, Teichman S, SGS742, a novel GABAB receptor antagonist, improves cognition in patients with mild cognitive impairment. Meeting of the American Association of Neurology, San Francisco, April 27, 2004, Poster P02.053. Olpe, 1979, Inhibition of nigral and neocortical cells by γ-hydroxybutyrate: a microiontophoretic investigation, Eur J Pharmacol, 53, 359, 10.1016/0014-2999(79)90460-6