Isoguvacine HCl (1,2,3,6-tetrahydropyridine-4-carboxylic acid) is a GABA (gamma-aminobutyric acid) agonist with limited conformational flexibility. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the post-synaptic GABA recognition site; that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA[1]. Isoguvacine, a GABAA receptor agonist, enhances substance P (SP) release in the spinal cord[2]. Bilateral microinjection of the GABAA receptor agonist isoguvacine or the GABAB receptor agonist baclofen attenuated the AAR(adipose afferent reflex)[3]. Neurons in the pontine Kölliker-Fuse nucleus (KF) were inhibited with bilateral microinjections of isoguvacine (50-70 nl, 10 mm) to remove the post-inspiratory phase of respiration[4]. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently[5].
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