Gaba antagonists: convulsants and antidotes
Gamma-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the adult brain. And since everyone, including our brain, needs to relax from time to time for normal work, GABA maintains the activity and plasticity of the nervous system [1]. For example, GABA reduces the level of fear and anxiety.
Therefore, GABA antagonists most often exhibit a stimulating, sometimes convulsive, effect. And usually, GABA antagonists are used in science for experiments. For example, if as a result of the experiment, injections of GABA or a GABA agonist reduced the level of fear, then it is necessary to check whether this is precisely related to the effect on the GABA receptors. To confirm the hypothesis, the researchers will inject a suitable GABA inhibitor, and if an increase in fear is recorded, they will confirm that GABA reduces the level of fear [2]. Scientists are actively studying whether GABA and its agonists can help patients with autism, schizophrenia, Down syndrome and other neurodevelopmental disorders [1]. And in all such studies, GABA antagonists are needed.
But some GABA antagonists are used in medicine. For example, bilobalide is an anticonvulsant drug. The fact is that it interferes not only with the work of GABA, but also reduces the release of glutamate and, as a result, bilobalide acts as a neuroprotective agent [3]. Another GABA antagonist, flumazenil, is used as an antidote for benzodiazepine overdose. Because benzodiazepine stimulates exactly the GABA receptors, developing its sedative effect through them. Flumazenil prevents excess benzodiazepine from activating GABA receptors [4]. In addition, flumazenil helps people with benzodiazepine addiction and withdrawal symptoms [5].
It is very useful to have a library of GABA antagonists for investigating any of the many effects of GABA. You can purchase a large library of GABA antagonists right now on this site.
References
1. Tang, Xin, Rudolf Jaenisch, and Mriganka Sur. “The role of GABAergic signaling in neurodevelopmental disorders.” Nature Reviews Neuroscience 22.5 (2021): 290-307.
2. Chen, Xia, et al. “Human pharmacology of positive GABA-A subtype-selective receptor modulators for the treatment of anxiety.” Acta Pharmacologica Sinica 40.5 (2019): 571-582.
3. Johnston, Graham AR. “Advantages of an antagonist: bicuculline and other GABA antagonists.” British journal of pharmacology 169.2 (2013): 328-336.
4. Hood, Sean David, et al. “Benzodiazepine dependence and its treatment with low dose flumazenil.” British journal of clinical pharmacology 77.2 (2014): 285-294.
5. Hulse, Gary, et al. “Novel indications for benzodiazepine antagonist flumazenil in GABA mediated pathological conditions of the central nervous system.” Current pharmaceutical design 21.23 (2015): 3325-3342.
Alexander Khazanov
Therefore, GABA antagonists most often exhibit a stimulating, sometimes convulsive, effect. And usually, GABA antagonists are used in science for experiments. For example, if as a result of the experiment, injections of GABA or a GABA agonist reduced the level of fear, then it is necessary to check whether this is precisely related to the effect on the GABA receptors. To confirm the hypothesis, the researchers will inject a suitable GABA inhibitor, and if an increase in fear is recorded, they will confirm that GABA reduces the level of fear [2]. Scientists are actively studying whether GABA and its agonists can help patients with autism, schizophrenia, Down syndrome and other neurodevelopmental disorders [1]. And in all such studies, GABA antagonists are needed.
But some GABA antagonists are used in medicine. For example, bilobalide is an anticonvulsant drug. The fact is that it interferes not only with the work of GABA, but also reduces the release of glutamate and, as a result, bilobalide acts as a neuroprotective agent [3]. Another GABA antagonist, flumazenil, is used as an antidote for benzodiazepine overdose. Because benzodiazepine stimulates exactly the GABA receptors, developing its sedative effect through them. Flumazenil prevents excess benzodiazepine from activating GABA receptors [4]. In addition, flumazenil helps people with benzodiazepine addiction and withdrawal symptoms [5].
It is very useful to have a library of GABA antagonists for investigating any of the many effects of GABA. You can purchase a large library of GABA antagonists right now on this site.
References
1. Tang, Xin, Rudolf Jaenisch, and Mriganka Sur. “The role of GABAergic signaling in neurodevelopmental disorders.” Nature Reviews Neuroscience 22.5 (2021): 290-307.
2. Chen, Xia, et al. “Human pharmacology of positive GABA-A subtype-selective receptor modulators for the treatment of anxiety.” Acta Pharmacologica Sinica 40.5 (2019): 571-582.
3. Johnston, Graham AR. “Advantages of an antagonist: bicuculline and other GABA antagonists.” British journal of pharmacology 169.2 (2013): 328-336.
4. Hood, Sean David, et al. “Benzodiazepine dependence and its treatment with low dose flumazenil.” British journal of clinical pharmacology 77.2 (2014): 285-294.
5. Hulse, Gary, et al. “Novel indications for benzodiazepine antagonist flumazenil in GABA mediated pathological conditions of the central nervous system.” Current pharmaceutical design 21.23 (2015): 3325-3342.
Alexander Khazanov
