Chemistry:Isoguvacine

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Isoguvacine is a GABAA receptor agonist used in scientific research.[1] It is a highly charged zwitterion and is unable to enter the central nervous system or produce central mediated effects.[2][3] There has been interest in centrally penetrant isoguvacine prodrugs for potential medical use.[3]

See also

References

  1. ↑ "Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures". Epilepsy Research 86 (2–3): 113–23. October 2009. doi:10.1016/j.eplepsyres.2009.05.008. PMID 19535226. 
  2. ↑ "Gaboxadol--a new awakening in sleep". Curr Opin Pharmacol 6 (1): 30–36. February 2006. doi:10.1016/j.coph.2005.10.004. PMID 16368265. "Early studies demonstrated that the highly charged zwitterions isoguvacine and P4S were unable to enter the CNS or exert any pharmacological activity, whereas muscimol and (to an even larger extent) gaboxadol produced observable changes in behaviour after systemic application [25].". 
  3. ↑ 3.0 3.1 "GABA receptor agonists: relationship between structure and biological activity in vivo and in vitro". GABA—Biochemistry and CNS Functions. Advances in Experimental Medicine and Biology. 123. Boston, MA: Springer US. 1979. pp. 303–321. doi:10.1007/978-1-4899-5199-1. ISBN 978-1-4899-5201-1. "Isoguvacine apparently does not easily penetrate the bloodbrain barrier after systemic administration. Hence, a variety of its derivatives have been developed as part of a systematic search for "pro-drugs" of isoguvacine. The goal of this approach is to develop a non-toxic derivative of isoguvacine, which easily penetrates into the brain after systemic administration and which is subsequently hydrolyzed therein to give isoguvacine. A "pro-drug" of isoguvacine which meets these pharmacokinetic requirements may be of pharmacological and possibly of therapeutic interest." 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

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