TY - JOUR AU - Rahman, MM AU - Ozoe, F AU - Ozoe, Y PY - 2021/03/29 Y2 - 2024/03/28 TI - Competitive antagonism of housefly γ-aminobutyric acid receptors by iminopyridazine butanoic acids JF - Bangladesh Journal of Scientific and Industrial Research JA - Bangladesh J. Sci. Ind. Res. VL - 56 IS - 1 SE - Articles DO - 10.3329/bjsir.v56i1.52690 UR - https://www.banglajol.info/index.php/BJSIR/article/view/52690 SP - 9-16 AB - <p>The competitive antagonistic activities of a series of gabazine (3) based 3-substituted iminopyridazine butanoic acid analogs [4-(3-aryl/heteroaryl-1,6-dihydro- 6-iminopyridazin-1-yl) butanoic acid hydrochlorides] 4a-4k (Figure 1) were examined at housefly (<em>Musca domestica</em>) GABA receptors expressed in <em>Xenopus </em>oocytes using two-electrode voltage-clamp (TEVC) technique. The 4-biphenylyl analog 4e exhibited the highest inhibition (approximately 68%) of GABA-induced currents at 100 μM with an IC50 value of 40.81 ± 3.89 μM. The 2-naphthyl analog 4h was the second most active compound with approximately 48% inhibition. The 4-biphenylyl analog 4e demonstrated competitive antagonism of housefly GABA receptors. Ligand docking studies into the binding site of housefly GABA receptor homology model predicted that the aromatic 3-substituents are tolerable in the pyridazine ring. The results presented in this paper about GABA receptor competitive antagonists may helpful for design and development of GABA receptor related insecticides.</p><p><em>Bangladesh J. Sci. Ind. Res.</em><strong>56(1),</strong> 9-16, 2021</p> ER -