(-)-Bicuculline methobromide - CAS 73604-30-5
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
GABA Receptor
(-)-Bicuculline methobromide is the methobromide salt of (+)-bicuculline, which is a potent antagonist of GABAA receptors.
Brife Description:
GABAA receptor antagonist
≥98% by HPLC
[R-(R,S)]-5-(6,8-Dihydro-8-oxofuro[3,4-e]-1,3-benzodioxol-6-yl)-5,6,7,8-tetrahydro-6,6-dimethyl-1,3-dioxolo[4,5-g]isoquinolinium bromide
Canonical SMILES:
1.Enhancement of 3H-phenytoin binding by diazepam and (+)bicuculline.
Okazaki MM;Madras BK;Livingston KE;Spero L;Burnham WM Life Sci. 1983 Aug 1;33(5):409-14.
3H-Phenytoin binding to the particulate fraction of rat wholebrain homogenate was studied using the filter assay technique. It was found that diazepam and (+)bicuculline methobromide caused a concentration-dependent enhancement of the total binding of 3H-phenytoin, whereas GABA and (-)bicuculline methobromide (the inactive bicuculline isomer) had no effect. In subsequent competition experiments (labelled versus unlabelled phenytoin), it was found that the presence of a potentiating concentration of diazepam transformed the biphasic phenytoin competition isotherm into a simple curve with a Hill coefficient of approximately one, and a Ki of 110 nM.
2.The contribution of adenosine to paired-pulse inhibition in the normal and disinhibited hippocampal slice.
Higgins MJ;Stone TW Eur J Pharmacol. 1996 Dec 19;317(2-3):215-23.
The effects of the adenosine receptor antagonist 1,3-dimethyl-8-cyclopentylxanthine (cyclopentyltheophylline) and the enzyme adenosine deaminase have been examined on paired-pulse inhibition between orthodromic evoked field potentials in the CA1 region of the normal and disinhibited hippocampal slice. In the presence of the GABAA receptor antagonist (-)-bicuculline methobromide, cyclopentyltheophylline suppressed homosynaptic paired-pulse inhibition between stimuli 300 ms apart. Slices treated with (-)-bicuculline and cyclopentyltheophylline together tended to develop spontaneous burst potentials. In slices in which a surgical cut isolated the CA1 and CA3 areas, thereby preventing the development of bursts in CA1, the effect on paired-pulse inhibition was lessened but was still apparent. Adenosine deaminase, in the presence of (-)-bicuculline showed the same effect as cyclopentyltheophylline, decreasing substantially the amount of paired-pulse inhibition. These results suggest that adenosine may contribute to homosynaptic paired-pulse inhibition in disinhibited slices. For comparison, we also examined the effect of cyclopentyltheophylline in normal ((-)-bicuculline-free) slices. At 100 nM, cyclopentyltheophylline increased reversibly the size of orthodromically evoked synaptic population potentials in the CA1 region of the slices and also reduced reversibly the degree of homosynaptic paired-pulse inhibition between two stimuli delivered only 30 ms apart.
3.The antiallodynic effect of Neurotropin is mediated via activation of descending pain inhibitory systems in rats with spinal nerve ligation.
Okazaki R;Namba H;Yoshida H;Okai H;Miura T;Kawamura M Anesth Analg. 2008 Sep;107(3):1064-9. doi: 10.1213/ane.0b013e31817e7a59.
BACKGROUND: ;Neurotropin, a nonprotein extract isolated from inflamed skin of rabbits inoculated with vaccinia virus, is widely used in Japan to treat chronic pain such as neuropathic pain. Although some studies have been conducted on the mechanism of the antiallodynic action of Neurotropin, this mechanism has yet to be adequately clarified.;METHODS: ;The left fifth lumbar nerve of rats was tightly ligated with silk sutures under pentobarbital anesthesia. Mechanical allodynia was confirmed by measuring the hindpaw withdrawal threshold in response to application of von Frey filaments. Behavioral tests were performed at 28 days after nerve ligation. Neurotropin was administered IV, intrathecally or intracerebroventricularly in L5 spinal nerve ligation (L5-SNL) rats. We examined the effects of noradrenergic, serotonergic and gamma-aminobutyric acid (GABA)ergic antagonists on the antiallodynic action of Neurotropin in L5-SNL rats. Yohimbine hydrochloride (yohimbine) was used as an alpha(2) adrenoceptor antagonist, ketanserin tartrate (ketanserin) as a 5-HT(2A) receptor antagonist, MDL72,222 as a 5-HT(3) receptor antagonist, (-)-bicuculline methobromide (bicuculline) as a GABA(A) receptor antagonist, and CGP35,348 as a GABA(B) receptor antagonist, and intrathecally injected.
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CAS 73604-30-5 (-)-Bicuculline methobromide

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