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Binding of dexetimide and levetimide to [3H](+)pentazocine- and [3H]1,3-Dl(2-tolyl)guanidine-defined σ recognition sites
- Source :
- Life Sciences. 49:PL135-PL139
- Publication Year :
- 1991
- Publisher :
- Elsevier BV, 1991.
-
Abstract
- The potent antimuscarinic benzetimide and its resolved stereoisomers dexetimide and levetimide were tested for their affinities at σ sites labelled by [ 3 H](+)pentazocine or [ 3 H]1,3-di(2-tolyl)guanidine. Levetimide was a potent and stereoselective inhibitor of [ 3 H](+)pentazocine binding, with a K i of 2.2 nM, while dexetimide was nine-fold less potent (K i = 19 nM). Dexetimide and levetimide potently inhibited [ 3 H]DTG binding although without stereoselectivity (K i values of 65 and 103 nM, respectively). Levetimide may be a useful tool with which to investigate σ recognition sites and σ subtypes.
- Subjects :
- Male
Agonist
Pentazocine
medicine.drug_class
Stereochemistry
Guinea Pigs
Levetimide
BENZETIMIDE
Binding, Competitive
Guanidines
General Biochemistry, Genetics and Molecular Biology
Radioligand Assay
chemistry.chemical_compound
Dexetimide
medicine
Animals
Receptors, sigma
General Pharmacology, Toxicology and Pharmaceutics
Guanidine
Cerebral Cortex
Myocardium
General Medicine
Receptors, Muscarinic
Affinities
chemistry
Receptors, Opioid
Stereoselectivity
medicine.drug
Subjects
Details
- ISSN :
- 00243205
- Volume :
- 49
- Database :
- OpenAIRE
- Journal :
- Life Sciences
- Accession number :
- edsair.doi.dedup.....46a4ad6ea6c42a375cb858a754d9503b