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GABAa agonists

KCNQ2/KCNQ3 Epilepsy retigabine (also GABAa agonist), BMS-204352... [Pg.995]

Figure 16.7 The structure of some established antiepileptic drugs (AEDs) and some newer ones. Note that while the structures of phenytoin and ethosuximide are similar and also close to that of phenobarbitone, they are effective in different forms of epilepsy. Vigabatrin, progabide and gabapentin are clearly related to GABA. Muscimol is a GABAa agonist but is not an effective antiepileptic drug... Figure 16.7 The structure of some established antiepileptic drugs (AEDs) and some newer ones. Note that while the structures of phenytoin and ethosuximide are similar and also close to that of phenobarbitone, they are effective in different forms of epilepsy. Vigabatrin, progabide and gabapentin are clearly related to GABA. Muscimol is a GABAa agonist but is not an effective antiepileptic drug...
Table 9 Efficacy and rat pharmacokinetic data for fluorinated GABAa agonists... Table 9 Efficacy and rat pharmacokinetic data for fluorinated GABAa agonists...
THIP (Gaboxadol) An Intriguing Example of a GABAa Agonist Exhibiting a Novel Pharmacological Profile... [Pg.88]

If only a low level of receptor activation is required in order to obtain a full response, one would predict that receptor desensitization would be a smaller problem with THIP, muscimol, and other GABAa agonists used as hypnotics. In an animal study, Lancel and Langebartels showed that 5-d treatment with THIP produced sustained effects on sleep parameters, whereas a benzodiazepine in a similar paradigm induced tolerance-like effects after only 5 d of treatment (52). Accepting that only... [Pg.90]

Faulhaber, J., Steiger, A., and Lancel, M. (1997) The GABAA agonist THIP produces slow wave sleep and reduces spindling activity in NREM sleep in humans. Psychopharmacology (Berl.) 130,285-291. [Pg.93]

The EEG effects of valerian are most concordant with those of tiagabine, a GABA uptake inhibitor used to treat epilepsy. Tiagabine also increases slow-wave sleep, but unlike valerian has little or no effect on REM (Lancel et al. 1998). GABAA agonists also tend to have this effect. [Pg.221]

Lancel M, Faulhaber J. (1996). The GABAA agonist THIP (gaboxadol) increases non-REM sleep and enhances delta activity in the rat. Neuroreport. 7(13) 2241-45. [Pg.498]

Akirav, I., Raizel, H., and Maroun, M. (2006). Enhancement of conditioned fear extinction by infusion of the GABAA agonist muscimol into the rat prefrontal cortex and amygdala. Eur.J. Neurosci 23,... [Pg.105]

Garant, D. S., Xu, S. G., Sperber, E. F., Moshe, S. L. (1995). Age-related differences in the effects of GABAA agonists microin-jected into rat substantia nigra Pro- and anticonvulsant actions. Epilepsia, 36, 960-965. [Pg.103]

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See also in sourсe #XX -- [ Pg.215 ]

See also in sourсe #XX -- [ Pg.995 , Pg.1036 ]



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