GABAb antagonists

Waldmeier, P. C. (1991) The GABAb antagonist, CGP 35348, antagonizes the effects of baclofen, gamma-butyrolactone and HA 966 on rat striatal dopamine synthesis. Naunyn Schmiedebergs Arch. Pharmacol. 343,173-178. 

Many examples in the glutamate antagonist series and in the GABAb antagonists... 

Non-planar sulfur or phosphorous-derived acidic functions The most extensive use of phosphonates was made in the design of amino acid neurotransmitter antagonists such as glutamate and GABAb antagonists. ... 

Froestl, W., Furet, P., Hall, R.G., Mickel, S.J., Strub, D., et al. (1993) GABAb antagonists novel CNS-active compounds. Perspectives in Medicinal Chemistry, pp. 259-272. VHC, Weinheiin. 

Fig. 18.2 Conjunctive approach in drug design. The attachment of two benzylic groups and a hydroxyi in S-configuration changes a GABAb receptor agonist into a GABAb antagonist, similarly the H2-histaminergic agonist impromidine is the result of a conjunctive approach applied to histamine. ...

Fiydenvang K, Hansen JJ, Krogsgaard-Larsen P, Mitrovic A, Tran H, Drew CA, Johnston GAR. GABAb antagonists resolution, absolute stereochemistry, and pharmacology of (R)-and (5)-phaclofen. Chirality 1994 6(7) 583-589. 

In contrast to the metabotropic effects described for presynaptic kainate receptors in CA1 (90,94), the effects of kainate in CA3 appear to be mediated by direct depolarization of the presynaptic terminals. The kainate-induced facilitation is not sensitive to antagonists of other receptors (e.g., GABAb), and can be mimicked by elevating the extracellular potassium concentration (77,100). It has been proposed that the facilitation is owing to increased calcium influx that is induced by modest depolarization of the terminals by kainate receptors, whereas a strong depolarization, in response to activation of a larger receptor population, causes the sodium channels to inactivate and thereby depresses transmission (77,84,88,100-102). 

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