5-amino-1-(2,6-dichloro-4-trifluoromethyl-phenyl)-3-[3H3]-methylsulfanyl-1H-pyrazole-4-carbonitrile (CTOM): synthesis and characterization of a novel and selective insect GABA receptor radioligand |
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| Authors: | Meegalla Sanath K Doller Dario Silver Gary M Wisnewski Nancy Soll Richard M Dhanoa Dale |
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| Institution: | 3-Dimensional Pharmaceuticals, Inc., 665 Stockton Drive, Suite 104, Exton, PA 19341, USA. meegalla@3dp.com |
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| Abstract: | Pyrazole 2a is a novel, potent ligand for insect GABA receptors obtained from housefly head membrane preparations (K(i)=8 nM). It is 500-fold selective against the mammalian receptor (mouse brain preparations). Its specifically tritiated version (2b) was synthesized by reduction of disulfide 10 with NaBH(4) followed by alkylation with 3H(3)]-CH(3)I. |
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