GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects.

@article{Krogsgaardlarsen2000GABAUI,
  title={GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects.},
  author={Povl Krogsgaard-larsen and Bente Fr{\o}lund and Karla Frydenvang},
  journal={Current pharmaceutical design},
  year={2000},
  volume={6 12},
  pages={
          1193-209
        }
}
In the mid seventies a drug design programme using the Amanita muscaria constituent muscimol (7) as a lead structure, led to the design of guvacine (23) and (R)-nipecotic acid (24) as specific GABA uptake inhibitors and the isomeric compounds isoguvacine (10) and isonipecotic acid (11) as specific GABAA receptor agonists. The availability of these compounds made it possible to study the pharmacology of the GABA uptake systems and the GABAA receptors separately. Based on extensive cellular and… CONTINUE READING
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