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Bicuculline methiodide, (-)-
Chemical Name:[R-(R*,S*)]-5-(6,8-Dihydro-8-oxofuro[3,4-e]-1,3-benzodi
oxol-6-yl)-5,6,7,8-tetrahydro-6,6-dimethyl-1,3-dioxolo[
4,5-g]isoquinolinium iodide
Biological Activity:
Methiodide form of classical GABAA
receptor antagonist (+)-bicuculline (Cat. No. 0130). More water-soluble and
stable. Non-GABA receptor-mediated actions reported.
Olsenet al (1976) Studies on the neuropharmacological activity
of bicuculline and related compounds. Brain Res. 102 283. Seutin
and Johnson (1999) Recent advances in the pharmacology of quaternary salts
of bicuculline. TiPS 20 268. Chanet al (2006)
Blockade of GABA(A) receptors in the ventromedial hypothalamus further
stimulates glucagon and sympathoadrenal but not the
hypothalamo-pituitary-adrenal response to hypoglycemia. Diabetes 55
1080.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.