Interactions of pentamethylenetetrazole and tetrazole analogues with the picrotoxinin site of the benzodiazepine-gaba receptor-ionophore complex

Ramanjaneyulu, R.; Ticku, Maharaj K.

doi:10.1016/0014-2999(84)90282-6

Cited by 271 publications

(118 citation statements)

References 23 publications

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“…It probably acts on GABA receptor and blocks the picrotoxin sensitive site. 29 It blocks GABA transmission in the brain. 30 GABA is an inhibitory neurotransmitter in the CNS.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of effect of aqueous extract of leaves of Calotropis procera in pentylenetetrazole induced seizures in rats

Ramachandra

Shenoy

Madhyastha

et al. 2016

Int J Basic Clin Pharmacol

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“…It probably acts on GABA receptor and blocks the picrotoxin sensitive site. 29 It blocks GABA transmission in the brain. 30 GABA is an inhibitory neurotransmitter in the CNS.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of effect of aqueous extract of leaves of Calotropis procera in pentylenetetrazole induced seizures in rats

Ramachandra

Shenoy

Madhyastha

et al. 2016

Int J Basic Clin Pharmacol

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“…its mechanism of action has not yet been fully clar ified. This agent has been reported to interact with the benzodiazepine--y-aminobutyric acid (GAB A) receptor or ionophore complex (MacDonald and Barker, 1977;Ramanjaneyulu and Ticku, 1984).…”

Section: Postnatal Evolution Of Lcbfmentioning

confidence: 99%

Effects of Pentylenetetrazol-Induced Status Epilepticus on Local Cerebral Blood Flow in the Developing Rat

Vasconcelos

Boyet

Koziel

et al. 1995

J Cereb Blood Flow Metab

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Summary:The quantitative autoradiographic e4Cl iodoantipyrine technique was applied to measure the ef fects of a 30-min period of pentylenetetrazol (PTZ) induced status epilepticus (SE) on local cerebral blood flow (LCBF) in rats 10 (PlO), 14 (PI4), 17 (P17), and 21 (P21) days after birth. The animals received repetitive, timed injections of subconvulsive doses of PTZ until SE was reached. At PIO, SE induced a 32 to 184% increase in the rates of LCBF affecting all structures studied. In PI4-and PI7 PTZ-treated rats, LCBF values significantly in creased in two-thirds of the structures belonging to all systems studied and were not changed by SE in the pa rietal cortex, dorsal hippocampus, and dentate gyrus. At P2I, rates of LCBF were still increased in 48 of the 73 structures studied; however, LCBF values were de creased by SE in most cortical areas, the hippocampus, Severe neonatal and infantile seizures are associ ated with poor neurological outcome, including hemiplegias, mental retardation, extended intellec tual impairment, alteration of cognitive function, and lesional epilepsies, in later life (Aicardi and Chevrie, 1970;Aicardi, 1977;Cull, 1988; Legido et aI., 1991).Increases in cerebral blood flow (CBF) accom pany epileptic seizure discharges in humans and ex perimental animals (Penfield et aI., 1939; Plum et aI., 1968;Meldrum and Nilsson, 1976; Horton et aI., 1980). In adults, the greatest increases in blood flow occur in the hippocampus, thalamus, and neocortex (Horton et aI., 1980). Blood flow rises within secReceived December 27, 1993; final revision received April 7, 1994; accepted May 3, 1994. Address correspondence and reprint requests to Dr. A. Pereira de Vasconcelos at Centre de Neurochimie, 5 rue Blaise Pascal, F-67084 Strasbourg Cedex, France.Abbreviations used: GABA, ,),-aminobutyric acid; lAP, io doantipyrine; LCBF, local cerebral blood flow; LCMRgl c , local cerebral metabolic rate for glucose; NO, nitric oxide; PIO, 10 days after birth, etc.; PTZ, pentylenetetrazol; SE, status epilep ticus. 270and the dentate gyrus. CBF and cerebral metabolic rate for glucose (CMRglc) remained coupled in both controls and PTZ-exposed rats. Our results show that changes in LCBF with seizures are age dependent. At the most im mature ages, PlO and PI4, both LCBF and local CMRglc (LCMRglc) values are largely increased by long-lasting seizures. At PI7 and P2I, the blood flow response to SE becomes more heterogeneous, with specific decreases in the hippocampus and cortex at P2I. The absence of mis match between LCBF and LCMRglc in PTZ-exposed rats at all ages may explain at least partly why the immature brain is more resistant to seizure-induced brain damage than the adult brain.

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“…Although animal models based on PTZ have still been widely used for drug screening, the mechanism by which PTZ elicits its action has not been completely understood. One generally accepted mechanism by which PTZ exerts its action is by acting as an antagonist at the picrotoxin sensitive site of GABAA receptor complex (Ramanjaneyulu and Ticku, 1984). GABA is a principal inhibitory neurotransmitter in the mammalian central nervous system, producing inhibitory post-synaptic potentials in both feedforward and feedback circuits.…”

Section: Discussionmentioning

confidence: 99%

Anticonvulsant Effect of Artemisia capillaris Herba in Mice

Woo¹,

Yoon²,

Peña³

et al. 2011

Biomolecules and Therapeutics

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In the present study, the anticonvulsant effects of Artemisia capillaris Herba (AC) and its major constituent, esculetin (ECT), were tested and the mechanism studied. Locomotion, Myorelaxation, motor coordination and electroshock seizure experiment were conducted in mice. To identify the anticonvulsant mechanism effect of this drug, chemical-induced seizure in mice and the ionic movement in neuroblastoma cells were also observed. The ethanol extract of AC was orally administered to mice 30 min. prior to testing and ECT was intraperitoneally injected. AC and ECT treatment did not change locomotor activities as well as activities on the rota-rod, which indicates that they did not cause a sedative and myorelaxation effect. AC and ECT treatment increased threshold of convulsion induced by electroshock. AC treatment also inhibited convulsion induced by pentylenetetrazole. In the case of strychnine however, only high dose of AC treatment inhibited convulsion. AC and ECT treatment increased the Cl − infl ux into the intracellular area in a dose-dependent manner. On the other hand, bicuculline, a GABA antagonist, inhibited the Cl − infl ux induced by AC and ECT. These results indicate that ECT induces the anticonvulsive effect of AC extract through the GABAergic neuron.

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Interactions of pentamethylenetetrazole and tetrazole analogues with the picrotoxinin site of the benzodiazepine-gaba receptor-ionophore complex

Cited by 271 publications

References 23 publications

Evaluation of effect of aqueous extract of leaves of Calotropis procera in pentylenetetrazole induced seizures in rats

Evaluation of effect of aqueous extract of leaves of Calotropis procera in pentylenetetrazole induced seizures in rats

Effects of Pentylenetetrazol-Induced Status Epilepticus on Local Cerebral Blood Flow in the Developing Rat

Anticonvulsant Effect of Artemisia capillaris Herba in Mice

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