Therefore, the different entities of the GABA system have been major targets for the development of drugs that are therapeutically active against these diseases. Among these drugs, the benzodiazepines may constitute one of the most important drug discoveries of modern pharmacology. View chapterExplore ...
In this report, the action of GABA agonists and antagonists is investigated both iontophoretically and intravenously on the trigeminal nucleus model. This technique permitted us to differentiate the direct effect of these drugs on the trigeminal neurons from the action on neurons elsewhere in the ...
Additional psychotropic drugs that are known to exert pain relief are GABA agonists [Blackburn-Munro G., et al., Curr Pharm Des. 2005; 11(23):2961-76]. Hence, the first chemical moiety may alternatively be a GABA agonist. Examples of GABA agonists are described hereinbelow. Conjugates of ...
WO/2002/018327 March, 2002 GUANIDINOBENZAMIDES AS MC4-R AGONISTS WO/2002/028345 April, 2002 ALDEHYDE-RELEASING COMPOUNDS WO/2002/028411 April, 2002 COMPOUNDS FOR SUSTAINED RELEASE OF ORALLY DELIVERED DRUGS WO/2002/028827 April, 2002 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, PHARMACEUTICAL COM...
(30 µM, Sigma, Denmark) and baclofen (10 µM, Sigma, Denmark) were used as agonists of the GABAAand GABABreceptors, respectively. Stock solutions were stored in appropriate aliquots at -20oC prior and diluted in ACSF to final concentrations before use, and all drugs were applied via ...
Jason L Niehaus1 and Julie A Kauer*,1 1Department of Molecular Pharmacology, Physiology and Biotechnology, Brown University, Providence, RI, USA Drugs of abuse usurp the mechanisms underlying synaptic plasticity in areas of the brain, a process that may contribute to the development of addiction....
Channel modulating drugs The activity of GABAAreceptors is modulated by subtype-selective agonists and antagonists belonging to different chemical families such as benzodiazepines or barbiturates and including anesthetic, anxiolytic or antiepileptic drugs. ...
diversity of GABAARs, the native isoforms have to be identified by their localization in the brain and by their pharmacology. In heterologous expression systems, channels require the presence of α, β, and γ subunits in order to mimic the full repertoire of native receptor responses to drugs,...
Differential interactions of GABA agonists, depressant and convulsant drugs with [35S]-t-butylbicyclophosphorothionate binding sites in cortex and cerebellum. Pharmacol. Biochem. Behav. 21, 151- 158.Ticku, M. K., and R. Ramanjaneyulu (1984) Differential interactions of GABA agonists, depressant...
Thus, a number of agents having sufficient pharmacological activity have been tested, either as GABA agonists or antagonists, or for their ability to release GABA from the CNS neurons. At best, these approaches have resulted in a trade off between improvement of transport across the blood-brain ...