Binding of dexetimide and levetimide to [3H](+)pentazocine- and [3H]1,3-di(2-tolyl)guanidine-defined sigma recognition sites. |
| |
Authors: | D L DeHaven-Hudkins R L Hudkins |
| |
Institution: | Department of Enzymology and Receptor Biochemistry, Sterling Research Group, Malvern, PA 19355-1314. |
| |
Abstract: | The potent antimuscarinic benzetimide and its resolved stereoisomers dexetimide and levetimide were tested for their affinities at sigma sites labelled by 3H](+)pentazocine or 3H]1,3-di(2-tolyl)guanidine. Levetimide was a potent and stereoselective inhibitor of 3H](+)pentazocine binding, with a Ki of 2.2 nM, while dexetimide was nine-fold less potent (Ki = 19 nM). Dexetimide and levetimide potently inhibited 3H]DTG binding although without stereoselectivity (Ki values of 65 and 103 nM, respectively). Levetimide may be a useful tool with which to investigate sigma recognition sites and sigma subtypes. |
| |
Keywords: | |
|
|