From Wikipedia, the free encyclopedia
Chemical compound
ROD-188 is a
sedative drug that was structurally derived from the
GABAA
antagonist
bicuculline by a team at Roche.
[1] Unlike bicuculline, ROD-188 acts as an
agonist at GABAA receptors, being a positive allosteric modulator acting at a novel binding site distinct from those of
benzodiazepines ,
barbiturates or
muscimol , with its strongest effect produced at the α6β2γ2 subtype of the GABAA receptor.
[2] ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.
[3]
[4]
See also
References
^
US 6649626 , "N-substituted 1-(lactone) isoquinolones for treating nervous disorders"
^ Thomet U, Baur R, Razet R, Dodd RH, Furtmüller R, Sieghart W, Sigel E (October 2000).
"A novel positive allosteric modulator of the GABA(A) receptor: the action of (+)-ROD188" . British Journal of Pharmacology . 131 (4): 843–850.
doi :
10.1038/sj.bjp.0703558 .
PMC
1572371 .
PMID
11030736 .
^ Sigel E, Baur R, Furtmueller R, Razet R, Dodd RH, Sieghart W (June 2001). "Differential cross talk of ROD compounds with the benzodiazepine binding site". Molecular Pharmacology . 59 (6): 1470–1477.
doi :
10.1124/mol.59.6.1470 .
PMID
11353808 .
^ Ramerstorfer J, Furtmüller R, Sarto-Jackson I, Varagic Z, Sieghart W, Ernst M (January 2011).
"The GABAA receptor α+β-interface: a novel target for subtype selective drugs" . The Journal of Neuroscience . 31 (3): 870–877.
doi :
10.1523/JNEUROSCI.5012-10.2011 .
PMC
3182524 .
PMID
21248110 .
S2CID
1989995 .
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ROD-188
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