Convulsant/depressant site of action at the allosteric benzodiazepine-gaba receptor-ionophore complex

Ticku, Maharaj K.; Maksay, Gábor

doi:10.1016/0024-3205(83)90630-6

Cited by 163 publications

(37 citation statements)

References 76 publications

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“…24) Barbiturates interact with GABA receptors and modulate GABA-ergic effects. 25,26) Many hypnotic, antianxiety and anti-epilepsy drugs prolong pentobarbitalinduced sleeping time. We were interested in whether sanjoinine A prolonged pentobarbital-induced sleeping behaviors via the GABA-ergic systems.…”

Section: Discussionmentioning

confidence: 99%

Sanjoinine A Isolated from Zizyphi Spinosi Semen Augments Pentobarbital-Induced Sleeping Behaviors through the Modification of GABA-ergic Systems

Han

Eun

et al. 2007

Biological & Pharmaceutical Bulletin

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Section: Discussionmentioning

confidence: 99%

Sanjoinine A Isolated from Zizyphi Spinosi Semen Augments Pentobarbital-Induced Sleeping Behaviors through the Modification of GABA-ergic Systems

Han

Eun

et al. 2007

Biological & Pharmaceutical Bulletin

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“…More recently, bemegride has been shown to inhibit the binding of TBPS to the GABAA receptor (Ticku & Maksay, 1983;Ticku & Rastogi, 1986). Experiments were therefore made to test whether bemegride could be used as a specific barbiturate antagonist.…”

Section: Gaba-evoked Whole-cell Currents and Blockade With Bicucullinementioning

confidence: 99%

Actions of steroids and bemegride on the GABAA receptor of mouse spinal neurones in culture

Mistry¹,

Cottrell²

1990

Experimental Physiology

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SUMMARYThe effects of a synthetic and an endogenous steroid were studied on the GABAA receptors of isolated mouse spinal neurones, maintained in culture. Low doses of alphaxalone reversibly increased GABA-evoked whole-cell currents. Alphaxalone at higher doses (10-50 'M), when pressure ejected onto spinal neurones, also directly evoked a membrane chloride current. Such currents were reversibly suppressed by bicuculline (a GABAA antagonist) and enhanced by phenobarbitone. 5,/-Pregnan-3a-ol-20-one, a progesterone metabolite, dose-dependently potentiated the amplitude of GABA-evoked whole-cell currents. The mechanism of potentiation was examined at the single-channel level using outside-out patches from spinal neurones. The main action of the steroid on the GABAA receptor appears to be similar to that found for barbiturates, in that they prolonged GABA-activated bursts of channel openings. Bemegride had an antagonistic action on the GABAA receptor, suppressing both GABA-and pentobarbitone-evoked whole-cell currents to similar extents.

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“…The pharmacophore model proposed in this study shares much with a number of other models which have been proposed for the GABA convulsant site (Soloway, 1965;Milbrath et al, 1979;Klunk et al, 1983;Ticku and Maksay, 1983;Ozoe and Matsumura, 1986;Matsumura et al, 1987;Wong and Andrews, 1989;Ozoe et al, 1990;Watanabe et al, 1990;Mullin, 1991;Paramonov et al, 1990;Calder et al, 1993;Lees and Calder, 1996;Akamatsu et al, 1997). There are some differences however, particularly with respect to the placement of the isopropenyl group of picrotoxinin in this model compared to the model of Akamatsu (Akamatsu eta/., 1997).…”

Section: Discussionmentioning

confidence: 68%

Polycyclic dinitriles: a novel class of potent GABAergic insecticides provides a new radioligand, [3H]BIDN

Rauh

Holyoke

Kleier

et al. 1997

Invertebrate Neuroscience

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The polycyclic dinitriles are a potent class of insecticides which are non-competitive GABA (gamma-aminobutyric acid) antagonists acting at the convulsant site. Comparison with other classes of GABA convulsant site ligands using molecular modelling has shown significant structural similarities. We have developed a pharmacophore model which unifies this class and some previous classes of GABA convulsants. Key pharmacophore elements are a polarizable functionality separated by a fixed distance from two H-bond accepting elements. This model is based on information from X-ray crystal structures and Sybyl using the Tripos force field. Using this pharmacophore model, numerous structural modifications were explored to enhance understanding of structure-activity relationships at the GABA receptor convulsant site of insects and mammals. A radiolabelled bicyclic dinitrile, [3H]BIDN [3H]3,3-bis-trifluoromethyl-bicyclo[2,2,1]heptane-2,2-dicarbonitrile+ ++), was prepared from this area of chemistry and was used as a probe for the interaction of polycyclic dinitriles at the target site.

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Convulsant/depressant site of action at the allosteric benzodiazepine-gaba receptor-ionophore complex

Cited by 163 publications

References 76 publications

Sanjoinine A Isolated from Zizyphi Spinosi Semen Augments Pentobarbital-Induced Sleeping Behaviors through the Modification of GABA-ergic Systems

Sanjoinine A Isolated from Zizyphi Spinosi Semen Augments Pentobarbital-Induced Sleeping Behaviors through the Modification of GABA-ergic Systems

Actions of steroids and bemegride on the GABAA receptor of mouse spinal neurones in culture

Polycyclic dinitriles: a novel class of potent GABAergic insecticides provides a new radioligand, [3H]BIDN

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