| Design and Synthesis of Photoaffinity Probe Candidates for the GABA-gated Chloride Channel |
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| 引用本文： | 刘尚钟 LI Qing-X.. Design and Synthesis of Photoaffinity Probe Candidates for the GABA-gated Chloride Channel[J]. 中国化学, 2006, 24(10): 1435-1438. DOI: 10.1002/cjoc.200690269 |
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| 作者姓名： | 刘尚钟 LI Qing-X. |
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| 作者单位： | Department of Applied Chemistry China Agricultural University，Beijing 100094，China，Department of Molecular Biosciences and Bioengineering，University of Hawaii at Manoa，Honolulu，Hawaii 96822，USA |
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| 基金项目： | Project supported by the National Basic Research Program of China(No.2003CB114405)，Hawaii Heptacblor Education,Research Foundation,USDA-ARS award number 58-5320-3-315. |
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| 摘 要： | In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel,new photoaf-finity probe candidates based on 5e-t-butyl-2e-[4-(substituted-propynyl)phenyl]-1,3-dithiane for the noncompetitiveblocker(NCB)site of the γ-aminobutyric acid(GABA)-gated chloride channel were designed and synthesized,andtheir potency as an inhibitor on NCB was measured by 4'-ethynyl-4-n-[2,3-~3H_2]-propylbicycloorthobenzoate(~3HEBOB)assay.The synthesized compounds showed high inhibition activities with half maximum inhibition concen-trations(IC_(50))of lower than 35 nmol/L and were very stable in binding conditions as well photoreacted quickly at300 nm light.These new compounds are expected to be good photoaffinity labeling probes if radioisotope iodine isincorporated.
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| 关 键 词： | 光亲和势 GABA受体 1 3-二噻烷 氯化物 γ-氨基丁酸 |
| 收稿时间： | 2005-11-21 |
| 修稿时间： | 2005-11-212006-06-21 |
Design and Synthesis of Photoaffinity Probe Candidates for the GABA-gated Chloride Channel |
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| LIU Shang-Zhong, LI Qing-X.. Design and Synthesis of Photoaffinity Probe Candidates for the GABA-gated Chloride Channel[J]. Chinese Journal of Chemistry, 2006, 24(10): 1435-1438. DOI: 10.1002/cjoc.200690269 |
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| Authors: | LIU Shang-Zhong LI Qing-X. |
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| Affiliation: | 1.Department of Applied Chemistry, China Agricultural University, Beijing 100094, China; 2.Department of Molecular Biosciences and Bioengineering, University of Hawaii at Manoa, Honolulu, Hawaii 96822, USA |
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| Abstract: | In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel, new photoaffinity probe candidates based on 5e‐t‐butyl‐2e‐[4‐(substituted‐propynyl)phenyl]‐1,3‐dithiane for the noncompetitive blocker (NCB) site of the γ‐aminobutyric acid (GABA)‐gated chloride channel were designed and synthesized, and their potency as an inhibitor on NCB was measured by 4′‐ethynyl‐4‐n‐[2,3‐3H2]‐propylbicycloorthobenzoate (3H EBOB) assay. The synthesized compounds showed high inhibition activities with half maximum inhibition concentrations (IC50) of lower than 35 nmol/L and were very stable in binding conditions as well photoreacted quickly at 300 nm light. These new compounds are expected to be good photoaffinity labeling probes if radioisotope iodine is incorporated. |
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| Keywords: | photoaffinity labeling GABA receptor 1 3-dithiane |
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