Pharmacological characterization and molecular diversity of GABA receptors
Kinya Kuriyama, Masaaki Hirouchi
Abstract
Open-access reader
Kinya Kuriyama, Masaaki Hirouchi
Abstract
Open-access reader
The GABA receptors are classified into two major subtypes, GABAA and GABAB. The many inhibitory central acting drugs such as benzodiazepines and barbiturates affect the GABAA receptors. The GABAA receptors consist of several subunits and form C1 channel. The multiple combinations of subunits exhibit varieties of pharmacological actions as GABAA and benzodiazepine receptors. On the other hand, the GABAB receptor, one of metabotropic receptors, is a 80 kDa protein coupled with Gi families and the presence of subtypes in the GABAB receptor is proposed from various biochemical or pharmacological studies. The therapeutic applications of GABAB receptor agonists and antagonists are attempted in the cognitive disorders, epilepsy, depression and pain.
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The GABA receptors are classified into two major subtypes, GABAA and GABAB. The many inhibitory central acting drugs such as benzodiazepines and barbiturates affect the GABAA receptors. The GABAA receptors consist of several subunits and form C1 channel. The multiple combinations of subunits exhibit varieties of pharmacological actions as GABAA and benzodiazepine receptors. On the other hand, the GABAB receptor, one of metabotropic receptors, is a 80 kDa protein coupled with Gi families and the presence of subtypes in the GABAB receptor is proposed from various biochemical or pharmacological studies. The therapeutic applications of GABAB receptor agonists and antagonists are attempted in the cognitive disorders, epilepsy, depression and pain.
Key concepts: GABAB receptor, GABAA receptor, Metabotropic receptor, Receptor, GABAA-rho receptor, Class C GPCR, Pharmacology, Chemistry