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研究领域

GABA receptors Nicotinic acetylcholine receptors The rapid advances in molecular biology and genetics have contributed towards the discovery and isolation of a large number of receptors and proteins that may be targets to treat various disease states. My team focuses on studying GABA and nicotinic acetylcholine receptors and their involvement in anxiety, sleep disorders and learning and memory. Structure-activity relationship (SAR) studies involving structural variations of both the agents and their receptor targets (termed complementary structure-activity studies) play important roles in drug design and development. Of particular focus is the structure-function studies of GABA and nicotinic receptors using site-directed mutagenesis in combination with reactive probes help identify amino acids that are important in the binding and function of receptors. In addition, animal models to evaluate the effects of important ligands establish a link between the in vitro and in vivo effects. Such studies are vital to the discovery of drugs that interact selectively with particular receptor subtypes and in receptors that may have inheritable mutations.

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Ahring, J., Bang, L., Jensen, M., Strobaek, D., Hartiadi, L., Collins, M., Absalom, N. (2016). A pharmacological assessment of agonists and modulators at alpha-4-beta-2-gamma-2 and alpha-4-beta-2-gamma GABAA receptors: The challenge in comparing apples with oranges. Pharmacological Research, 111, 563-576. [More Information] Lee, H., Absalom, N., Hanrahan, J., van Nieuwenhuijzen, P., Ahring, J., Collins, M. (2016). A pharmacological characterization of GABA, THIP and DS2 at binary α4β3 and β3δ receptors: GABA activates β3δ receptors via the β3(+)δ(-) interface. Brain Research, 1644, 222-230. [More Information] Khan, I., Karim, N., Ahmad, W., Abdelhalim, A., Collins, M. (2016). GABA-A Receptor Modulation and Anticonvulsant, Anxiolytic, and Antidepressant Activities of Constituents from Artemisia indica Linn. Evidence-Based Complementary and Alternative Medicine, 2016, 1-12. [More Information] Hartiadi, L., Ahring, J., Chebib, M., Absalom, N. (2016). High and low GABA sensitivity alpha4beta2delta GABAA receptors are expressed in Xenopus laevis oocytes with divergent stoichiometries. Biochemical Pharmacology, 103, 98-108. [More Information] Carland, J., Yamamoto, I., Hanrahan, J., Abdel-Halim, H., Lewis, T., Absalom, N., Chebib, M. (2015). A Hydrophobic Area of the GABA p1 Receptor Containing Phenylalanine 124 Influences Both Receptor Activation and Deactivation. Journal of Molecular Neuroscience, 55(2), 305-313. [More Information] Abdelhalim, A., Karim, N., Chebib, M., Aburjai, T., Khan, I., Johnston, G., Hanrahan, J. (2015). Antidepressant, Anxiolytic and Antinociceptive Activities of Constituents from Rosmarinus Officinalis. Journal of Pharmacy and Pharmaceutical Sciences, 18(4), 448-459. Naffaa, M., Chebib, M., Hibbs, D., Hanrahan, J. (2015). Comparison of templates for homology model of rho1 GABAC receptors: More insights to the orthosteric binding site's structure and functionality. Journal of Molecular Graphics and Modelling, 62, 43-55. [More Information] Ahring, J., Olsen, J., Nielsen, E., Peters, D., Pedersen, M., Rohde, L., Kastrup, J., Shahsavar, A., Indurthi Venkata, D., Chebib, M., Balle, T., et al (2015). Engineered alpha4beta2 nicotinic acetylcholine receptors as models for measuring agonist binding and effect at the orthosteric low-affinity alpha4-alpha4 interface. Neuropharmacology, 92, 135-145. [More Information] Karim, N., Irshad, S., Khan, I., Mohammad, A., Anis, I., Shah, M., Khan, I., Chebib, M. (2015). GABAA receptor modulation and neuropharmacological activities of viscosine isolated from Dodonaea viscosa (Linn). Pharmacology, Biochemistry and Behavior, 136, 64-72. [More Information] Neumann, S., Shields, N., Balle, T., Chebib, M., Clarkson, A. (2015). Innate Immunity and Inflammation Post-Stroke: An alpha7-Nicotinic Agonist Perspective. International Journal of Molecular Sciences, 16(12), 29029-29046. [More Information] Hanrahan, J., Chebib, M., Johnston, G. (2015). Interactions of flavonoids with ionotropic GABA receptors. Advances in Pharmacology, 72, 189-200. [More Information] Bowen, M., Peters, S., Absalom, N., Chebib, M., Neumann, I., McGregor, I. (2015). Oxytocin prevents ethanol actions at δ subunitcontaining GABAA receptors and attenuates ethanolinduced motor impairment in rats. Proceedings of the National Academy of Sciences of the United States of America (PNAS), 112(10), 3104-3109. [More Information] Hellyer, S., Indurthi Venkata, D., Balle, T., Runder-Varga, V., Selwood, A., Tyndall, J., Chebib, M., Rhodes, L., Kerr, S. (2015). Pinnatoxins E, F and G target multiple nicotinic receptor subtypes. Journal of Neurochemistry, 135(3), 479-491. [More Information] Absalom, N., Yamamoto, I., O'Hagan, D., Hunter, L., Collins, M. (2015). Probing the Mode of Neurotransmitter Binding to GABA Receptors Using Selectively Fluorinated GABA Analogues. Australian Journal of Chemistry, 68(1), 23-30. [More Information] Chua, H., Absalom, N., Hanrahan, J., Viswas, R., Chebib, M. (2015). The Direct Actions of GABA, 2’-Methoxy-6-Methylflavone and General Anaesthetics at β3γ2L GABAA Receptors: Evidence for Receptors with Different Subunit Stoichiometries. PloS One, 10(10), 1-19. [More Information] Gallagher, R., Chebib, M., Balle, T., McLeod, M. (2015). Thiol-Reactive Analogues of Galanthamine, Codeine, and Morphine as Potential Probes to Interrogate Allosteric Binding within Nicotinic Acetylcholine Receptors. Australian Journal of Chemistry, 68(12), 1834-1841. [More Information] Beltrán González, A., Pomata, P., Goutman, J., Gasulla, J., Chebib, M., Calvo, D. (2014). Benzodiazepine modulation of homomeric GABAAp1 receptors: Differential effects of diazepam and 4'-chlorodiazepam. European Journal of Pharmacology, 743, 24-30. [More Information] Abdelhalim, A., Chebib, M., Aburjai, T., Johnston, G., Hanrahan, J. (2014). GABAA Receptor Modulation by Compounds Isolated from Salvia triloba L. Advances in Biological Chemistry, 4(2), 148-159. [More Information] Blednov, Y., Benavidez, J., Black, M., Leiter, C., Osterndoff-Kahanek, E., Johnson, D., Borghese, C., Hanrahan, J., Johnston, G., Chebib, M., et al (2014). GABAA Receptors Containing p1 Subunits Contribute to In Vivo Effects of Ethanol in Mice. PloS One, 9(1), 1-16. [More Information] Hall, B., Karim, N., Chebib, M., Johnston, G., Hanrahan, J. (2014). Modulation of Ionotropic GABA Receptors by 6-Methoxyflavanone and 6-Methoxyflavone. Neurochemical Research, 39, 1068-1078. [More Information]

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