2005
DOI: 10.1111/j.1527-3458.2005.tb00049.x
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Clinical Potential of GABAB Receptor Modulators

Abstract: Metabotropic gamma-aminobutyric acid(B) (GABAB) receptors for the major inhibitory transmitter GABA, together with metabotropic glutamate (mGLuRs) receptors, the extracellular calcium-sensing receptors (CaSRs), some V2R pheromone receptors and T1R taste receptors, belong to the family of 3 G-protein-coupled receptors (GPCRs). GABAB receptors are known to control neuronal excitability and modulate synaptic neurotransmission, playing a very important role in many physiological activities. These receptors are wid… Show more

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Cited by 55 publications
(34 citation statements)
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References 95 publications
(116 reference statements)
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“…Hence they rather enhance the physiologic pattern of GABA B receptor activation, and so may have less adverse effects than ligands that alter all GABA B receptors. In agreement, allosteric modulators interfere less with locomotor activity (Ong and Kerr, 2005) and do not induce hypothermia (Jacobson and Cryan, 2008).…”
mentioning
confidence: 55%
“…Hence they rather enhance the physiologic pattern of GABA B receptor activation, and so may have less adverse effects than ligands that alter all GABA B receptors. In agreement, allosteric modulators interfere less with locomotor activity (Ong and Kerr, 2005) and do not induce hypothermia (Jacobson and Cryan, 2008).…”
mentioning
confidence: 55%
“…Consistent with these effects, the GABA B receptor agonist baclofen decreases nicotine priming-induced reinstatement of drug seeking [121]. While baclofen also reduces total cigarettes smoked per day and tobacco craving in human smokers [122], compliance is limited by adverse effects including cognitive impairments, sedation, muscle relaxation and tolerance [123]. In contrast, PAMs of GABA B receptors have fewer adverse effects than full agonists.…”
Section: Neurotransmitter Mechanisms Regulating Nicotine Seekingmentioning
confidence: 88%
“…The most predominant pharmacological effects of baclofen are its muscle relaxant, anti-nociceptive and anti-drug craving properties [9,10] as well as the reduction in cognitive behaviour [11]. Baclofen is used clinically for the treatment of spasticity associated with brain and spinal cord injuries [12], drug addiction and alcoholism [13,14], gastroesophageal reflux disease (GERD) [15], cancer pain [16] and overactive bladder [17][18][19].…”
Section: A Submicellar Liquid Chromatographic Methods For Quantitativementioning
confidence: 99%