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

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

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...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.4035-4037
Hauptverfasser: Meegalla, Sanath K, Doller, Dario, Silver, Gary M, Wisnewski, Nancy, Soll, Richard M, Dhanoa, Dale
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Insecta
Molecular Structure
Nitriles - chemical synthesis
Nitriles - pharmacokinetics
Pyrazoles - chemical synthesis
Pyrazoles - pharmacokinetics
Radioligand Assay
Receptors, GABA - chemistry
Receptors, GABA - metabolism
Structure-Activity Relationship
Tritium
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Beschreibung
Zusammenfassung: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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2003.08.042