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Excitatory Amino Acid Receptors and Afferent Synaptic Transmission in the Nucleus Tractus Solitarius
Published in I. Robin A. Barraco, Nucleus of the Solitary Tract, 2019
Michael C. Andresen, Mingyong Yang
Initially, we used two selective antagonists to try to identify the transmitter mediating this short-latency, tract-synched EPSP response in medial NTS neurons.36 AP5 (2-amino-5-phosphonovalerate) is one of the most selective NMDA receptor antagonists available and CNQX (6-cyano-7-nitro-quinoxaline-2,3-dione) selectively blocks non-NMDA receptors. Neurons were hyperpolarized (5 to 15 mV) to prevent spontaneous spiking and to allow observation of EPSPs without triggering spikes. EPSPs to low-frequency (0.5 Hz) repetitive tract stimulation were recorded before and during drug application. Increasing concentrations of antagonist were repeatedly applied to the surface of the slice for 1 to 2 min near where the tip of the microelectrode entered. Complete concentration-response relations were tested.
Fosamprenavir
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Suzanne M. Crowe, Christine Katlama, Robert Murphy
The benefits of the higher plasma concentrations with ritonavir boosting include improved inhibitory quotient, higher barrier against resistance, the feasibility of once-daily dosing, and improved virologic efficacy in selected persons with prior protease inhibitor exposure (Duval et al., 2002). The addition of ritonavir, however, is hampered by the side effects attributable to ritonavir (see Chapter 248, Ritonavir and cobicistat). Fosamprenavir was presented as a 465-mg tablet in the first phase II study. At doses of 1395 mg (three 465-mg tablets) and 1860 mg (four 465-mg tablets) twice daily for 28 days, fosamprenavir rapidly reduced plasma HIV-1 RNA concentrations by about 2 log copies/ml, and CD4+ cell counts increased by about 100 cells/mm3. This was similar to the antiviral effects of amprenavir 1200 mg twice daily. With these results, the 1395 mg twice-daily dose was selected for further development (Wood et al., 2004b). The GlaxoSmithKline (GSK) study APV 10006 demonstrated bioequivalence between the 465- and 700-mg tablets formulations, which led to the selection of 700-mg tablet formulation for further clinical trials.
Excitatory Amino Acids in Epilepsy
Published in Elling Kvamme, Glutamine and Glutamate in Mammals, 1988
Henry F. Bradford, Dale W. Peterson
A number of amino acid antagonists without selective or potent action at this receptor have been shown to be effective in other epilepsy models. As described above, d,l-APB and d,l-APV were shown to be anticonvulsant in the kindling model of epilepsy which, like the cobalt focus, was used to measure the antagonism of the local electrophysiological events at the focus as well as the overall convulsive components of the seizures. APB was far less active than APH or the closely related A1 antagonist APV on kindled amygdala seizures and the associated electrical afterdischarges.41,45 In contrast, kindled seizures arising in the hippocampus (which are of lesser severity) were blocked completely by APB in some animals.42,45 This action of APB in hippocampal kindling is likely to be related to the known suppression of synaptically mediated excitation in the hippocampus, which is caused by this antagonist.66
Molecular Mechanisms Associated with the Benefits of Variable Practice in Motor Learning
Published in Journal of Motor Behavior, 2020
Tércio Apolinário-Souza, Ana Flávia Santos Almeida, Natália Lelis-Torres, Juliana Otoni Parma, Grace Schenatto Pereira, Guilherme Menezes Lage
We administered the NMDA receptor antagonist intra-motor cortex (1 µg/µL). We injected the volume of 0.5 µl/side bilaterally by intracerebral microinfusion. To the drug administration, we contained the animals without anesthesia or sedation to prevent influences in motor behavior. We contained the animals for 30 s to place the injector cannula, which was followed by a 2 min injection. We conducted this process 10 min before practice on both days of the acquisition phase. Considering that the AP5 application was made straight to the M1, 10 min was sufficient for the drug to act (Morris, Anderson, Lynch, & Baudry, 1986). Finally, we anesthetized the animals with 3% isoflurane and euthanized them by cervical dislocation followed by decapitation. We removed the encephalon and preserved it in formaldehyde for 24 h, and then stored the encephalon in a 30% sucrose solution to posterior confirmation of cannula placement.
Heterogeneity in sociodemographic characteristics and cardiovascular risk factors at the initiation of a lifestyle intervention for obesity within Germany: an APV multicenter study on 40,942 children and adolescents
Published in Child and Adolescent Obesity, 2018
Barbara Bohn, Rainer Stachow, Ines Gellhaus, Johannes Matthias, Hans Lichtenstern, Reinhard W. Holl
Data from the German/Austrian/Switzerland Adiposity Patients Registry (APV) were used for the present analysis. APV is a standardized multicenter database for prospective documentation of anthropometric and metabolic parameters in overweight or obese children and adolescents and is used by centers specialized in pediatric obesity care (inpatient rehabilitation or outpatient). Anonymized data are transmitted from participating APV centers to Ulm, Germany, and aggregated into a cumulative database for clinical research and quality assurance [11]. Twice a year, implausible and inconsistent data are reported back to the centers for verification or correction. The APV initiative is authorized by the Ethics Committee of the University of Ulm, Germany.
Emerging concepts on the use of ketamine for chronic pain
Published in Expert Review of Clinical Pharmacology, 2020
Yunpeng Yang, Dermot P. Maher, Steven P. Cohen
NMDARs were first implicated in the development of a specific type of neuronal plasticity known as LTP in 1983 when the application of a newly discovered NMDAR antagonist, AP5, was noted to block the development of LTP in rodent brain slices[46]. Subsequent work found that spinal application of AP5 depressed aversive reactions to acute pain, and inhibited wind-up[47]. Intrathecal administration of NMDA was noted to increase biting and scratching behavior in mice, and resulted in hyperalgesic effects in tail-flick and hot-plate tests[48]. The same study also found that the nociceptive effects of NMDA could be inhibited by application of ‘phencyclidine receptor’ antagonists[48].