Agents that modify thiol groups have been shown to alter ligand binding at a variety of receptor sites. In addition, alkylation of sulfhydryls has been shown to block ion channel conductance. We studied the effects of thiol reagents on y-aminobutyric acid (GABA)-activated chloride flux (36Cl-) and [
✦ LIBER ✦
3H-tert-butylbicycloorthobenzoate — A new ligand for the GABAA-receptor gated ion channel
✍ Scribed by A. I. Golovko; G. A. Sofronov
- Publisher
- Springer US
- Year
- 1992
- Tongue
- English
- Weight
- 209 KB
- Volume
- 113
- Category
- Article
- ISSN
- 0007-4888
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## Abstract The preparation of [^3^H]‐labelled tert‐butyl 8‐chloro‐5,6‐dihydro‐5‐methyl‐6‐oxo‐4H‐imidazo[1,5‐a][1,4]benzodiazepine 3‐carboxylate (TCIB, 6), a high affinity ligands for the diazepam insensitive (DI) subtype of the benzodiazepine receptor (BZR) is described. Synthesis of [^3^H]TCIB wa