GABA receptors GABAb

A third class of GABA receptor (GABAb) is the G-protein-coupled receptor, which opens ion channels via intermediaries (G-proteins). 

GABAb receptors mediate the slow and prolonged physiological effects of the inhibitory neurotransmitter GABA. Functional GABAb receptors are comprised of two subunits, GABAbR1 and GABAbR2. Both subunits are G-protein-coupled receptors, which couple to the Gi/o family and are densely expressed at spinal nociceptive synapses. 

GABA is the most prominent inhibitory neurotransmitter in the mammalian nervous system and acts via GABA receptors. Activation of GABAb receptors by GABA released from local spinal interneurons (Fig. 1) negatively modulates nociceptive transmission in the spinal cord. Agonists at GABAb receptors... 

GABAa receptor An ion channel (ionotropic) receptor for GABA. The GABAb receptor is a Gj protein-coupled receptor. 

GABA receptors are divided into two main types GABAa and GABAB. inhibitory postsynaptic potentials in many areas of the brain have a fast and slow component. The fast component is mediated by GABAa receptors and the slow component by GABAB receptors. The difference in kinetics stems from the differences in coupling of the receptors to ion channels. GABAa... 

Zarrindast MR, Oveissi Y. GABA and GABAb receptor sites involvement in rat thermoregulation. Gen Pharmacol 1988 19(2) 223-6. 

Progabide is an antispasticity drug that is also used in the treatment of epilepsy (1). Together with its metabolites, it acts as an agonist at both GABA and GABAb receptors. 

CGP 35348 is a phosphinic acid derivative, a (GABAb) GABA receptor ANTAGONIST. It is used as a pharmacological tool, and shows ANTICONVULSANT / ANTIEPILEPTIC properties in animal models. 

TBPS (tert-butyl bicyclic thiophosphate) is a (GABAb) gaba receptor antagonist, used as a tool for studying binding sites of the mammalian CNS ( S labelled). It is a CNS stimulant and convulsant neurotoxin. 

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