Genomes and Genes
Summary: DITERPENES with three LACTONES and a unique tert-butyl group, which are found in GINKGO plants along with BILOBALIDES.
- Huang M, Qian Y, Guan T, Huang L, Tang X, Li Y. Different neuroprotective responses of Ginkgolide B and bilobalide, the two Ginkgo components, in ischemic rats with hyperglycemia. Eur J Pharmacol. 2012;677:71-6 pubmed publisher..These results suggested that CBF plays crucial roles during early stage of reperfusion in the presence of hyperglycemia. Administration of compound that improves CBF may have little effect in hyperglycemic stroke. ..
- Jones F, Chatterjee S, Davies J. Effects of bilobalide on amino acid release and electrophysiology of cortical slices. Amino Acids. 2002;22:369-79 pubmed..These results suggest that the neuroactive properties of bilobalide may be mediated by a reduction in excitatory amino acid neurotransmitter release. ..
- He N, Xie H, Collins X, Edeki T, Yan Z. Effects of individual ginsenosides, ginkgolides and flavonoids on CYP2C19 and CYP2D6 activity in human liver microsomes. Clin Exp Pharmacol Physiol. 2006;33:813-5 pubmed1. The effects of four individual ginsenosides (Rb1, Rb2, Rc and Rd), two ginkgolides (A and B) and one flavonoid (quercetin) on CYP2C19-dependent S-mephenytoin 4 cent-hydroxylation and CYP2D6-mediated bufuralol 1 cent-hydroxylation were ..
- Kiewert C, Kumar V, Hildmann O, Rueda M, Hartmann J, Naik R, et al. Role of GABAergic antagonism in the neuroprotective effects of bilobalide. Brain Res. 2007;1128:70-8 pubmed..We conclude that, while antagonism of GABA(A) receptors may contribute to bilobalide's neuroprotective effects, additional mechanisms must be postulated to fully explain bilobalide's actions. ..
- Huang S, Duke R, Chebib M, Sasaki K, Wada K, Johnston G. Ginkgolides, diterpene trilactones of Ginkgo biloba, as antagonists at recombinant alpha1beta2gamma2L GABAA receptors. Eur J Pharmacol. 2004;494:131-8 pubmedb>Ginkgolides A, B, and C are diterpene trilactones and active constituents of the 50:1 Ginkgo biloba leaf extract widely used in the symptomatic treatment of mild to moderate dementia...
- Teather L, Afonso V, Wurtman R. Inhibition of platelet-activating factor receptors in hippocampal plasma membranes attenuates the inflammatory nociceptive response in rats. Brain Res. 2006;1097:230-3 pubmed..These findings suggest that hippocampal plasma membrane PAF receptors, but not intracellular PAF binding sites, mediate tonic inflammatory pain processing in rats. ..
- Cirino G, Peers S, Wallace J, Flower R. A study of phospholipase A2-induced oedema in rat paw. Eur J Pharmacol. 1989;166:505-10 pubmed..The PAF-antagonist BN 52021, but not WEB2086, was an effective inhibitor. Degranulation of mast cells seem the most likely explanation for the inflammatory action of these enzymes in the rat paw. ..
- Wu Y, Wu Z, Butko P, Christen Y, Lambert M, Klein W, et al. Amyloid-beta-induced pathological behaviors are suppressed by Ginkgo biloba extract EGb 761 and ginkgolides in transgenic Caenorhabditis elegans. J Neurosci. 2006;26:13102-13 pubmed
- Liao H, Zheng Y, Li H, Peng G. Two new ginkgolides from the leaves of Ginkgo biloba. Planta Med. 2011;77:1818-21 pubmed publisher..The activities of the compounds were evaluated against platelet aggregation induced by platelet activating factor (PAF), and the preliminary structure-activity relationship was also discussed. ..
- Li Z, Ya K, Xiao Mei W, Lei Y, Yang L, Ming Q. Ginkgolides protect PC12 cells against hypoxia-induced injury by p42/p44 MAPK pathway-dependent upregulation of HIF-1alpha expression and HIF-1DNA-binding activity. J Cell Biochem. 2008;103:564-75 pubmed..In this study, we therefore investigated the effects of ginkgolides, the main constituent of the non-flavone fraction of EGb 761, on the content and activity of HIF-1alpha, a key ..
- He W, Qian Zhong M, Zhu L, Christopher Q, Du F, Yung W, et al. Ginkgolides mimic the effects of hypoxic preconditioning to protect C6 cells against ischemic injury by up-regulation of hypoxia-inducible factor-1 alpha and erythropoietin. Int J Biochem Cell Biol. 2008;40:651-62 pubmed..To find a safer preconditioning stimulus that is both practical and effective, we investigated whether ginkgolides are capable of preconditioning as hypoxia to protect C6 cells against ischemic injury...
- Li R, Chen B, Wu W, Bao L, Li J, Qi R. Ginkgolide B suppresses intercellular adhesion molecule-1 expression via blocking nuclear factor-kappaB activation in human vascular endothelial cells stimulated by oxidized low-density lipoprotein. J Pharmacol Sci. 2009;110:362-9 pubmed..In conclusion, ginkgolide B may decrease inflammatory responses induced by ox-LDL via blocking NF-kappaB signaling and inhibiting ROS generation in HUVECs. ..
- Tchantchou F, Lacor P, Cao Z, Lao L, Hou Y, Cui C, et al. Stimulation of neurogenesis and synaptogenesis by bilobalide and quercetin via common final pathway in hippocampal neurons. J Alzheimers Dis. 2009;18:787-98 pubmed publisher..Despite a recent report showing that EGb 761 was insufficient in prevent dementia, its constituents still warrant future investigation. ..
- Liu X, Zhao G, Yan Y, Bao L, Chen B, Qi R. Ginkgolide B reduces atherogenesis and vascular inflammation in ApoE(-/-) mice. PLoS ONE. 2012;7:e36237 pubmed publisher..The efficacy of ginkgolide B was similar to aspirin. These results provide direct evidence that ginkgolide B inhibits atherosclerosis, which may be associated with inhibition of the PI3K/Akt pathway in activated platelets. ..
- Huang S, Duke R, Chebib M, Sasaki K, Wada K, Johnston G. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464:1-8 pubmed..While bilobalide and picrotoxinin were clearly noncompetitive antagonists, the potency of bilobalide decreased at high GABA concentrations suggesting a component of competitive antagonism. ..
- Chandrasekaran K, Mehrabian Z, Spinnewyn B, Drieu K, Fiskum G. Neuroprotective effects of bilobalide, a component of the Ginkgo biloba extract (EGb 761), in gerbil global brain ischemia. Brain Res. 2001;922:282-92 pubmed..These results suggest that oral administration of bilobalide and EGb 761 protect against ischemia-induced neuron death and reductions in mitochondrial gene expression. ..
- Jaracz S, Strømgaard K, Nakanishi K. Ginkgolides: selective acetylations, translactonization, and biological evaluation. J Org Chem. 2002;67:4623-6 pubmed..These acetyl derivatives, as well as ginkgolides A and B acetates have been investigated for their ability to bind to a cloned platelet-activating factor (PAF) ..
- DeFeudis F. Bilobalide and neuroprotection. Pharmacol Res. 2002;46:565-8 pubmed..As multiple modes of action may apply to bilobalide, it could be useful in developing therapy for disorders involving cerebral ischemia and neurodegeneration. ..
- Zhang C, Tian X, Luo Y, Meng X. Ginkgolide B attenuates ethanol-induced neurotoxicity through regulating NADPH oxidases. Toxicology. 2011;287:124-30 pubmed publisher..Moreover, expression and activities of NADPH oxidases were down-regulated by GB. These results indicate that ethanol-induced neurotoxicity is ameliorated by GB mainly through regulating expression and activity of NADPH oxidases. ..
- Lau A, Yang G, Yap C, Chang T. Selective agonism of human pregnane X receptor by individual ginkgolides. Drug Metab Dispos. 2012;40:1113-21 pubmed publisher..In the present study, we investigated the effects of individual ginkgolides as single chemical entities on the function of human PXR (hPXR), human GR (hGR), and human CAR (hCAR)...
- He N, Cai H, Xie H, Collins X, Edeki T, Strom S. Induction of cyp3a in primary cultures of human hepatocytes by ginkgolides a and B. Clin Exp Pharmacol Physiol. 2007;34:632-5 pubmed..3. Compared with the vehicle control, ginkgolides A and B, at 30 micromol/L, significantly induced CYP3A protein expression (2...
- Jensen A, Begum N, Vogensen S, Knapp K, Gundertofte K, Dzyuba S, et al. Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007;50:1610-7 pubmedb>Ginkgolides are antagonists of the inhibitory ligand-gated ion channels for the neurotransmitters glycine and gamma-aminobutyric acid (GABA)...
- Kang S, Min J, Kim Y, Karigar C, Kim S, Goo G, et al. Effect of biotic elicitors on the accumulation of bilobalide and ginkgolides in Ginkgo biloba cell cultures. J Biotechnol. 2009;139:84-8 pubmed publisherThe effect of biotic elicitors on the production of bilobalide and ginkgolides in Ginkgo biloba cell suspension cultures was studied...
- Li X, Ma M, Scherban K, Tam Y. Liquid chromatography-electrospray mass spectrometric studies of ginkgolides and bilobalide using simultaneous monitoring of proton, ammonium and sodium adducts. Analyst. 2002;127:641-6 pubmedA liquid chromatographic-electrospray mass spectrometric method was developed for the determination of ginkgolides and bilobalide and was applied to the analysis of commercial products of Ginkgo biloba leaf extracts...
- Fang D, Ming Q, Li Z, Mei W, Ya K. Hypothermia attenuates protective effects of ginkgolides on astrocytes from ischemia/reperfusion injury. Neurochem Int. 2009;55:181-6 pubmed publisherThe neuroprotective roles of both hypothermia and ginkgolides have been well confirmed...
- Hawthorne R, Cromer B, Ng H, Parker M, Lynch J. Molecular determinants of ginkgolide binding in the glycine receptor pore. J Neurochem. 2006;98:395-407 pubmedb>Ginkgolides are potent blockers of the glycine receptor Cl- channel (GlyR) pore...
- Maclennan K, Darlington C, Smith P. The CNS effects of Ginkgo biloba extracts and ginkgolide B. Prog Neurobiol. 2002;67:235-57 pubmed..The aim of this review is to summarise and to critically evaluate the current evidence on the CNS effects of EGb-761 and ginkgolide B, with particular emphasis on the data relating to their neuroprotective effects. ..
- Esposito M, Carotenuto M. Ginkgolide B complex efficacy for brief prophylaxis of migraine in school-aged children: an open-label study. Neurol Sci. 2011;32:79-81 pubmed publisher..33 vs. 4.53 ± 3.96 attacks; p < 0.001). Our findings suggest that in childhood headache management, the use of alternative treatments must be considered not to evoke a placebo effect, but as soft therapy without adverse reactions. ..
- Huang S, Duke R, Chebib M, Sasaki K, Wada K, Johnston G. Mixed antagonistic effects of bilobalide at rho1 GABAC receptor. Neuroscience. 2006;137:607-17 pubmed..The mechanism of action of bilobalide at rho(1) GABA(C) receptors appears to be similar to that of the chloride channel blocker picrotoxinin. ..
- van Beek T. Ginkgolides and bilobalide: their physical, chromatographic and spectroscopic properties. Bioorg Med Chem. 2005;13:5001-12 pubmedb>Ginkgolides A, B, C, J, K, L and M and bilobalide are rare terpene trilactones that have been isolated from leaves and root bark of the Chinese tree Ginkgo biloba...
- Jensen A, Bergmann M, Sander T, Balle T. Ginkgolide X is a potent antagonist of anionic Cys-loop receptors with a unique selectivity profile at glycine receptors. J Biol Chem. 2010;285:10141-53 pubmed publisher..the functional properties of the compound were significantly different from those of the naturally occurring ginkgolides A, B, C, J, and M but similar to those of picrotoxin...
- D Andrea G, Bussone G, Allais G, Aguggia M, D Onofrio F, Maggio M, et al. Efficacy of Ginkgolide B in the prophylaxis of migraine with aura. Neurol Sci. 2009;30 Suppl 1:S121-4 pubmed publisher..Ginkgolide B is effective in reducing MA frequency and duration. The effect is clearly evident in the first bimester of treatment and is further enhanced during the second. ..
- Heads J, Hawthorne R, Lynagh T, Lynch J. Structure-activity analysis of ginkgolide binding in the glycine receptor pore. J Neurochem. 2008;105:1418-27 pubmed publisherb>Ginkgolides, active constituents of Ginkgo biloba extracts, potently block the glycine receptor chloride channel (GlyR)...
- Fang W, Deng Y, Li Y, Shang E, Fang F, Lv P, et al. Blood brain barrier permeability and therapeutic time window of Ginkgolide B in ischemia-reperfusion injury. Eur J Pharm Sci. 2010;39:8-14 pubmed publisher..In conclusion, Ginkgolide B could pass through BBB, especially after ischemia-reperfusion injury of brain, and might be therapeutically effective for ischemia/reperfusion injury of human brain...
- Yoshitake T, Yoshitake S, Kehr J. The Ginkgo biloba extract EGb 761(R) and its main constituent flavonoids and ginkgolides increase extracellular dopamine levels in the rat prefrontal cortex. Br J Pharmacol. 2010;159:659-68 pubmed publisher..This finding may be one of the mechanisms underlying the reported effects of G. biloba in improving cognitive function. ..
- Zhang S, Chen B, Wu W, Bao L, Qi R. Ginkgolide B reduces inflammatory protein expression in oxidized low-density lipoprotein-stimulated human vascular endothelial cells. J Cardiovasc Pharmacol. 2011;57:721-7 pubmed publisher..It seems that ginkgolide B possesses some pharmacological action on intracellular oxidative stress in association with the downregulation of Nox4 expression. ..
- Jaracz S, Malik S, Nakanishi K. Isolation of ginkgolides A, B, C, J and bilobalide from G. biloba extracts. Phytochemistry. 2004;65:2897-902 pubmedb>Ginkgolides A, B, C and J, together with bilobalide, are unique terpenoid components of the Ginkgo biloba tree. Due to similar chemical properties, their separation is quite tedious...
- Velasquez L, Aguilera J, Croxatto H. Possible role of platelet-activating factor in embryonic signaling during oviductal transport in the hamster. Biol Reprod. 1995;52:1302-6 pubmed..These results suggest that preimplantation hamster embryos produce PAF-like activity that mediates embryonic signaling to the oviduct as well as pregnancy-associated thrombocytopenia. ..
- Pérez Arellano J, Martin T, Lopez Novoa J, Sanchez M, Montero A, Jimenez A. BN 52021 (a platelet activating factor-receptor antagonist) decreases alveolar macrophage-mediated lung injury in experimental extrinsic allergic alveolitis. Mediators Inflamm. 1998;7:201-10 pubmed..Furthermore, antagonism of the PAF receptors notably decreases pulmonary parenchymatous lesion. These data suggest that lung lesions from acute EAA are partly mediated by local production of PAF. ..
- Tang Y, Huang B, Sun L, Peng X, Chen X, Zou X. Ginkgolide B promotes proliferation and functional activities of bone marrow-derived endothelial progenitor cells: involvement of Akt/eNOS and MAPK/p38 signaling pathways. Eur Cell Mater. 2011;21:459-69 pubmed..These ?ndings raise the intriguing possibility that GB may play an important role in the protection and revascularization of blood vessels. ..
- Yang Q, Fang W, Lv P, Geng X, Li Y, Sha L. Therapeutic neuroprotective effects of XQ-1H in a rat model of permanent focal cerebral ischemia. Pharmacology. 2012;89:1-6 pubmed publisher..In conclusion, the therapeutic time window of XQ-1H extends for up to 1 h after pMCAO, and treatment with XQ-1H exhibits potent neuroprotection that may be of value for the design of stroke therapies. ..
- Deng F, Zito S. Development and validation of a gas chromatographic-mass spectrometric method for simultaneous identification and quantification of marker compounds including bilobalide, ginkgolides and flavonoids in Ginkgo biloba L. extract and pharmaceutical prepa. J Chromatogr A. 2003;986:121-7 pubmed..was developed and validated for the simultaneous determination of seven major chemical markers (bilobalide, ginkgolides A, B, C, kaempferol, quercetin and isorhamnetin) in phytopharmaceuticals of Ginkgo biloba L...
- Chen J, Zhu L, Pan Y. [Ginkgolides induced ischemic tolerance and its possible molecular mechanism: experiment with rat pheochromocytoma cell line PC12]. Zhonghua Yi Xue Za Zhi. 2007;87:2432-5 pubmedTo explore the ischemic tolerance induced by Ginkgolides in PC12 cells and its possible molecular mechanism. An ischemic model was developed in PC12 cell line with deprivation of oxygen-glucose (OGD)...
- Ma S, Liu H, Jiao H, Wang L, Chen L, Liang J, et al. Neuroprotective effect of ginkgolide K on glutamate-induced cytotoxicity in PC 12 cells via inhibition of ROS generation and Ca(2+) influx. Neurotoxicology. 2012;33:59-69 pubmed publisher..Therefore, the present study supports the notion that ginkgolide K may be a promising neuroprotective agent for the treatment of cerebral ischemia disease. ..
- Li L, Zhao X, Fei X, Gu Z, Qin Z, Liang Z. Bilobalide inhibits 6-OHDA-induced activation of NF-kappaB and loss of dopaminergic neurons in rat substantia nigra. Acta Pharmacol Sin. 2008;29:539-47 pubmed publisher..NF-kappaB activation contributes to the 6-OHDA-induced loss of dopaminergic neurons, and the inhibition of the NF-kappaB pathway is likely to be involved in the neuroprotective effect of bilobalide. ..
- Zhang L, Xu J, Rong S, Xie B, Sun Z, Zhang Y, et al. The mixture of procyanidins extracted from the lotus seed pod and bilobalide ameliorates scopolamine-induced memory impairment in mice. Neurosci Bull. 2009;25:203-8 pubmed publisher..Co-treatment of LSPE and BIL can ameliorate scopolamine-induced learning and memory impairment in young mice. ..
- Hu W, Kinnaird A, Man R. Mechanisms of the coronary vascular effects of platelet-activating factor in the rat perfused heart. Br J Pharmacol. 1991;103:1097-102 pubmed..The ineffectiveness of PAF antagonists in blocking the vasodilatation produced by PAF is compatible with the concept that there may be multiple PAF receptors. ..
- Bussolino F, Silvagno F, Garbarino G, Costamagna C, Sanavio F, Arese M, et al. Human endothelial cells are targets for platelet-activating factor (PAF). Activation of alpha and beta protein kinase C isozymes in endothelial cells stimulated by PAF. J Biol Chem. 1994;269:2877-86 pubmed..These results suggest that activation of PKC alpha and beta is an important signal transduction pathway by which PAF activates endothelial monolayer and modify its function of barrier to macromolecules. ..
- Gui C, Zhu W, Chen G, Luo X, Liew O, Puah C, et al. Understanding the regulation mechanisms of PAF receptor by agonists and antagonists: molecular modeling and molecular dynamics simulation studies. Proteins. 2007;67:41-52 pubmed..The simulations revealed that binding of PAF to PAFR triggers the straightening process of the kinked helix VI, leading to its activated state. In contrast, binding of GB to PAFR locks PAFR in its inactive state. ..
- Yang Y, Ma X, Wang C, Han J, Lu Y, Xiang Y, et al. Effect of increased hepatic platelet activating factor and its receptor portal hypertension in CCl4-induced liver cirrhosis. World J Gastroenterol. 2006;12:709-15 pubmed..The upregulation of the PAF system contributes to hepatic hemodynamic and metabolic abnormalities in cirrhosis, and the increased release of PAF into the circulation has impacts on the systemic hemodynamics. ..
- Ahlemeyer B, Krieglstein J. Pharmacological studies supporting the therapeutic use of Ginkgo biloba extract for Alzheimer's disease. Pharmacopsychiatry. 2003;36 Suppl 1:S8-14 pubmed..the neuroprotective and anti-apoptotic ability of the main constituents of the non-flavone fraction, the ginkgolides A, B, C, J and bilobalide. In focal cerebral ischemia models, the administration of bilobalide (5-20 mg/kg, s...
- Chandrasekaran K, Mehrabian Z, Spinnewyn B, Chinopoulos C, Drieu K, Fiskum G. Bilobalide, a component of the Ginkgo biloba extract (EGb 761), protects against neuronal death in global brain ischemia and in glutamate-induced excitotoxicity. Cell Mol Biol (Noisy-le-grand). 2002;48:663-9 pubmed
- van Haeringen N, Verbey N, Van Delft J. Antagonists and inhibitors of lipid mediators in experimental inflammation of the cornea. J Ocul Pharmacol. 1993;9:365-72 pubmed..Prophylactic topical treatment with the poly-unsaturated fatty acids eicosapentaenoic acid and columbinic acid or a dietary supplement with fish oil showed less symptoms of keratitis in all respects. ..
- Laszlo F, Whittle B, Moncada S. Interactions of constitutive nitric oxide with PAF and thromboxane on rat intestinal vascular integrity in acute endotoxaemia. Br J Pharmacol. 1994;113:1131-6 pubmed..Such findings support the protective role of constitutively-formed NO, counteracting the injurious vascular actions of cytotoxic mediators released under pathological conditions. ..
- Xu J, Sun C, Ma H, Wang L, Zhang J, Zhang Y, et al. [Neuroprotective effect of extract of Ginkgo biloba against excitotoxicty compared with ginkgolide B in neuron cell of rat]. Zhongguo Zhong Yao Za Zhi. 2010;35:114-7 pubmed..The maximal protection of GB was achieved by pretreatment is superior to EGb761, so its precautionanary intervention to high-risk population could have more value. ..
- Gawron Gzella A, Marek P, Chanaj J, Matławska I. Comparative analysis of pharmaceuticals and dietary supplements containing extracts from the leaves of Ginkgo biloba L. Acta Pol Pharm. 2010;67:335-43 pubmed..Some of them satisfied applicable quality criteria (mainly preparation 8), however, the majority had reduced levels of therapeutic compounds (4, 6, 7, 11) and increased concentration of ginkgolic acids (4, 9, 10, 11). ..
- van Beek T, Montoro P. Chemical analysis and quality control of Ginkgo biloba leaves, extracts, and phytopharmaceuticals. J Chromatogr A. 2009;1216:2002-32 pubmed publisher..For the analysis of Ginkgo proanthocyanidins (7%) for instance, no reliable assays are yet existing. Finally the growing literature on pharmacokinetic and fingerprinting studies of Ginkgo is briefly summarised. ..
- Zhang C, Li M, Tang Y, Zhang Y, Shi M, Sheng L. [Extraction, isolation and purification for ginkgolide B]. Zhongguo Zhong Yao Za Zhi. 2010;35:1961-4 pubmed..Finally the crude crystals were recrystallized with isopropanol. The purity of the ginkgolide B recrystallization was 95%. The process was stable and easy to operate, which was suited to industrialized production. ..
- Li S, Zhang Y, Yang L. Improving effect of Ginkgolide B on mitochondrial respiration of ischemic neuron after cerebral thrombosis in tree shrewa. Chin Med J (Engl). 2007;120:1529-33 pubmed
- Xia S, Fang D, Hu C, Bi H, Yang Y, Di Y. Effect of BN52021 on NFkappa-Bp65 expression in pancreatic tissues of rats with severe acute pancreatitis. World J Gastroenterol. 2007;13:882-8 pubmed..BN52021 exerts therapeutic effects through reducing the expression level of NF-kappaBp65 protein in the early stage of SAP. ..
- Weakley S, Wang X, Mu H, Lu J, Lin P, Yao Q, et al. Ginkgolide A-gold nanoparticles inhibit vascular smooth muscle proliferation and migration in vitro and reduce neointimal hyperplasia in a mouse model. J Surg Res. 2011;171:31-9 pubmed publisher..GA-GNP reduce vascular SMC proliferation and migration in vitro through reduced activation of ERK1/2. Local treatment with GA-GNP in areas of arterial injury reduced neointimal hyperplasia and subsequent stenosis. ..
- Chan W. Ginkgolide B induces apoptosis and developmental injury in mouse embryonic stem cells and blastocysts. Hum Reprod. 2006;21:2985-95 pubmed..Our results reveal for the first time that ginkgolide B retards the proliferation and development of mouse ESCs and blastocysts in vitro and causes developmental injury in vivo. ..
- Kondratskaya E, Lishko P, Chatterjee S, Krishtal O. BN52021, a platelet activating factor antagonist, is a selective blocker of glycine-gated chloride channel. Neurochem Int. 2002;40:647-53 pubmed..This substance fails to affect AMPA and NMDA responses. It may be concluded that BN52021 inhibits glycine-gated Cl- channels by interacting with the pore region and does not compete for the strychnine-binding centre. ..