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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.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2003 Nov 17; Vol. 13 (22), pp. 4035-7. - Publication Year :
- 2003
-
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.
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 13
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 14592502
- Full Text :
- https://doi.org/10.1016/j.bmcl.2003.08.042