JPET

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Right arrow Citation Map
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Möhler, H.
Right arrow Articles by Rudolph, U.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Möhler, H.
Right arrow Articles by Rudolph, U.

Vol. 300, Issue 1, 2-8, January 2002

A New Benzodiazepine Pharmacology

H. Möhler , J. M. Fritschy and U. Rudolph

Institute of Pharmacology and Toxicology, University of Zurich, Zurich, Switzerland (H.M., J.M.F., U.R.); and Department of Applied Biosciences, Swiss Federal Institute of Technology, Zurich, Switzerland (H.M.)

Classical benzodiazepine drugs are in wide clinical use as anxiolytics, hypnotics, anticonvulsants, and muscle relaxants. They act by enhancing the gamma -aminobutyric acidA (GABAA) receptor function in the central nervous system. The pharmacological relevance of the multitude of structurally diverse GABAA receptor subtypes has only recently been identified. Based on an in vivo point mutation strategy, alpha 1-GABAA receptors were found to mediate sedation, anterograde amnesia, and part of the seizure protection, whereas alpha 2-GABAA receptors, but not alpha 3-receptors, mediate anxiolysis. Rational drug targeting to specific receptor subtypes has now become possible. Only restricted neuronal networks will be modulated by the new subtype-selective drugs. Promising new anxiolytics have already been developed. A new pharmacology of the benzodiazepine site is on the horizon.

0022-3565/02/3001-0002$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 2002 by The American Society for Pharmacology and Experimental Therapeutics


This article has been cited by other articles:


Home page
 J. Exp. Biol.Home page
D. M. Caspary, L. Ling, J. G. Turner, and L. F. Hughes
Inhibitory neurotransmission, plasticity and aging in the mammalian central auditory system
J. Exp. Biol., June 1, 2008; 211(11): 1781 - 1791.
[Abstract] [Full Text] [PDF]

Home page
 Cereb CortexHome page
A. B. Ali and A. M. Thomson
Synaptic {alpha}5 Subunit-Containing GABAA Receptors Mediate IPSPs Elicited by Dendrite-Preferring Cells in Rat Neocortex
Cereb Cortex, June 1, 2008; 18(6): 1260 - 1271.
[Abstract] [Full Text] [PDF]

Home page
 Drug Metab. Dispos.Home page
C. L. Shaffer, M. Gunduz, A. D. Vaz, K. Venkatakrishnan, and A. H. Burstein
Metabolism and Disposition of a {gamma}-Aminobutyric Acid Type A Receptor Partial Agonist in Humans
Drug Metab. Dispos., April 1, 2008; 36(4): 655 - 662.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
S. M. Hanson and C. Czajkowski
Structural Mechanisms Underlying Benzodiazepine Modulation of the GABAA Receptor
J. Neurosci., March 26, 2008; 28(13): 3490 - 3499.
[Abstract] [Full Text] [PDF]

Home page
 Cereb CortexHome page
J. Yamada, T. Furukawa, S. Ueno, S. Yamamoto, and A. Fukuda
Molecular Basis for the GABAA Receptor-Mediated Tonic Inhibition in Rat Somatosensory Cortex
Cereb Cortex, August 1, 2007; 17(8): 1782 - 1787.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
C. M. Schofield and J. R. Huguenard
GABA Affinity Shapes IPSCs in Thalamic Nuclei
J. Neurosci., July 25, 2007; 27(30): 7954 - 7962.
[Abstract] [Full Text] [PDF]

Home page
 Proc. Natl. Acad. Sci. USAHome page
H. J. Ng, E. R. Whittemore, M. B. Tran, D. J. Hogenkamp, R. S. Broide, T. B. Johnstone, L. Zheng, K. E. Stevens, and K. W. Gee
Nootropic {alpha}7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators
PNAS, May 8, 2007; 104(19): 8059 - 8064.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
J. C. Earnheart, C. Schweizer, F. Crestani, T. Iwasato, S. Itohara, H. Mohler, and B. Luscher
GABAergic Control of Adult Hippocampal Neurogenesis in Relation to Behavior Indicative of Trait Anxiety and Depression States
J. Neurosci., April 4, 2007; 27(14): 3845 - 3854.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
Y. H Raol, I. V Lund, S. Bandyopadhyay, G. Zhang, D. S Roberts, J. H Wolfe, S. J Russek, and A. R Brooks-Kayal
Enhancing GABAA Receptor {alpha}1 Subunit Levels in Hippocampal Dentate Gyrus Inhibits Epilepsy Development in an Animal Model of Temporal Lobe Epilepsy.
J. Neurosci., November 1, 2006; 26(44): 11342 - 11346.
[Abstract] [Full Text] [PDF]

Home page
 J. Physiol.Home page
V. Di Lazzaro, F. Pilato, M. Dileone, F. Ranieri, V. Ricci, P. Profice, P. Bria, P. A. Tonali, and U. Ziemann
GABAA receptor subtype specific enhancement of inhibition in human motor cortex
J. Physiol., September 15, 2006; 575(3): 721 - 726.
[Abstract] [Full Text] [PDF]

Home page
 Arch Gen PsychiatryHome page
J. H. Krystal, J. Staley, G. Mason, I. L. Petrakis, J. Kaufman, R. A. Harris, J. Gelernter, and J. Lappalainen
{gamma}-Aminobutyric Acid Type A Receptors and Alcoholism: Intoxication, Dependence, Vulnerability, and Treatment.
Arch Gen Psychiatry, September 1, 2006; 63(9): 957 - 968.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurophysiol.Home page
G. A. Prenosil, E. M. Schneider Gasser, U. Rudolph, R. Keist, J.-M. Fritschy, and K. E. Vogt
Specific Subtypes of GABAA Receptors Mediate Phasic and Tonic Forms of Inhibition in Hippocampal Pyramidal Neurons
J Neurophysiol, August 1, 2006; 96(2): 846 - 857.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurophysiol.Home page
S. S. Kumar, X. Wen, Y. Yang, and P. S. Buckmaster
GABAA Receptor-Mediated IPSCs and {alpha}1 Subunit Expression Are Not Reduced in the Substantia Nigra Pars Reticulata of Gerbils With Inherited Epilepsy
J Neurophysiol, April 1, 2006; 95(4): 2446 - 2455.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
R. E. Petroski, J. E. Pomeroy, R. Das, H. Bowman, W. Yang, A. P. Chen, and A. C. Foster
Indiplon Is a High-Affinity Positive Allosteric Modulator with Selectivity for {alpha}1 Subunit-Containing GABAA Receptors
J. Pharmacol. Exp. Ther., April 1, 2006; 317(1): 369 - 377.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
Y. Zhang, A. L. Rodriguez, and P. J. Conn
Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes
J. Pharmacol. Exp. Ther., December 1, 2005; 315(3): 1212 - 1219.
[Abstract] [Full Text] [PDF]

Home page
 J. Physiol.Home page
V. Di Lazzaro, F. Pilato, M. Dileone, P. A. Tonali, and U. Ziemann
Dissociated effects of diazepam and lorazepam on short-latency afferent inhibition
J. Physiol., November 15, 2005; 569(1): 315 - 323.
[Abstract] [Full Text] [PDF]

Home page
 FocusHome page
D. J. Buysse, A. Germain, D. Moul, and E. A. Nofzinger
Insomnia
Focus, October 1, 2005; 3(4): 568 - 584.
[Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
P. H. Wu, W. Poelchen, and W. R. Proctor
Differential GABAB Receptor Modulation of Ethanol Effects on GABAA Synaptic Activity in Hippocampal CA1 Neurons
J. Pharmacol. Exp. Ther., March 1, 2005; 312(3): 1082 - 1089.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
A. C. Foster, M. A. Pelleymounter, M. J. Cullen, D. Lewis, M. Joppa, T. K. Chen, H. P. Bozigian, R. S. Gross, and K. R. Gogas
In Vivo Pharmacological Characterization of Indiplon, a Novel Pyrazolopyrimidine Sedative-Hypnotic
J. Pharmacol. Exp. Ther., November 1, 2004; 311(2): 547 - 559.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
S. K. Sullivan, R. E. Petroski, G. Verge, R. S. Gross, A. C. Foster, and D. E. Grigoriadis
Characterization of the Interaction of Indiplon, a Novel Pyrazolopyrimidine Sedative-Hypnotic, with the GABAA Receptor
J. Pharmacol. Exp. Ther., November 1, 2004; 311(2): 537 - 546.
[Abstract] [Full Text] [PDF]

Home page
 J. Biol. Chem.Home page
J. Simon, H. Wakimoto, N. Fujita, M. Lalande, and E. A. Barnard
Analysis of the Set of GABAA Receptor Genes in the Human Genome
J. Biol. Chem., October 1, 2004; 279(40): 41422 - 41435.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurophysiol.Home page
P. I. Ortinski, C. Lu, K. Takagaki, Z. Fu, and S. Vicini
Expression of Distinct {alpha} Subunits of GABAA Receptor Regulates Inhibitory Synaptic Strength
J Neurophysiol, September 1, 2004; 92(3): 1718 - 1727.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
J. Liang, E. Cagetti, R. W. Olsen, and I. Spigelman
Altered Pharmacology of Synaptic and Extrasynaptic GABAA Receptors on CA1 Hippocampal Neurons Is Consistent with Subunit Changes in a Model of Alcohol Withdrawal and Dependence
J. Pharmacol. Exp. Ther., September 1, 2004; 310(3): 1234 - 1245.
[Abstract] [Full Text] [PDF]

Home page
 Proc. Natl. Acad. Sci. USAHome page
C. Kopp, U. Rudolph, K. Low, and I. Tobler
Modulation of rhythmic brain activity by diazepam: GABAAreceptor subtype and state specificity
PNAS, March 9, 2004; 101(10): 3674 - 3679.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
E. Sanna, M. C. Mostallino, F. Busonero, G. Talani, S. Tranquilli, M. Mameli, S. Spiga, P. Follesa, and G. Biggio
Changes in GABAA Receptor Gene Expression Associated with Selective Alterations in Receptor Function and Pharmacology after Ethanol Withdrawal
J. Neurosci., December 17, 2003; 23(37): 11711 - 11724.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurosci.Home page
A. Bacci, U. Rudolph, J. R. Huguenard, and D. A. Prince
Major Differences in Inhibitory Synaptic Transmission onto Two Neocortical Interneuron Subclasses
J. Neurosci., October 22, 2003; 23(29): 9664 - 9674.
[Abstract] [Full Text] [PDF]

Home page
 NEJMHome page
J. A. Campagna, K. W. Miller, and S. A. Forman
Mechanisms of Actions of Inhaled Anesthetics
N. Engl. J. Med., May 22, 2003; 348(21): 2110 - 2124.
[Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
R. T. Robinson, B. C. Drafts, and J. L. Fisher
Fluoxetine Increases GABAA Receptor Activity through a Novel Modulatory Site
J. Pharmacol. Exp. Ther., March 1, 2003; 304(3): 978 - 984.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
S. A. G. Visser, F. L. C. Wolters, P. H. van der Graaf, L. A. Peletier, and M. Danhof
Dose-Dependent EEG Effects of Zolpidem Provide Evidence for GABAA Receptor Subtype Selectivity in Vivo
J. Pharmacol. Exp. Ther., March 1, 2003; 304(3): 1251 - 1257.
[Abstract] [Full Text] [PDF]

Home page
 J. Neurophysiol.Home page
E. Ramadan, Z. Fu, G. Losi, G. E. Homanics, J. H. Neale, and S. Vicini
GABAA Receptor beta 3 Subunit Deletion Decreases alpha 2/3 Subunits and IPSC Duration
J Neurophysiol, January 1, 2003; 89(1): 128 - 134.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
M. P. Mascia, F. Biggio, L. Mancuso, S. Cabras, P. L. Cocco, G. Gorini, A. Manca, C. Marra, R. H. Purdy, P. Follesa, et al.
Changes in GABAA Receptor Gene Expression Induced by Withdrawal of, but Not by Long-Term Exposure to, Ganaxolone in Cultured Rat Cerebellar Granule Cells
J. Pharmacol. Exp. Ther., December 1, 2002; 303(3): 1014 - 1020.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 2002 by the American Society for Pharmacology and Experimental Therapeutics.