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3-(1-Indolinyl)benzylamines: a new class of analgesic agents
- Source :
- Journal of medicinal chemistry. 28(1)
- Publication Year :
- 1985
-
Abstract
- An extensive series of 3-(1-indolinyl)benzylamines and related compounds was synthesized and tested for analgesic activity. After a detailed study of structure-activity relationships, 3-(1-indolinyl)benzylamine (2b) was selected for further investigation as the most interesting member of this novel class of compounds. It was active in both the phenylquinone writhing and tail-flick assays for analgesic activity. No motor deficits were observed in the rotorod test, and 2b was found to be free of any other effects on the central nervous system. The compound did not bind to opiate receptors, since it was inactive in inhibiting the stereospecific binding of [3H]naloxone in rat brain homogenates. Thus, 3-(1-indolinyl)benzylamine represents a novel analgesic with an unusual chemical structure and biological profile.
- Subjects :
- Analgesics
Indoles
Bicyclic molecule
Stereochemistry
Naloxone
Chemical structure
Analgesic
Central nervous system
Quinones
Pain
Biological activity
(+)-Naloxone
Binding, Competitive
chemistry.chemical_compound
Mice
Benzylamine
medicine.anatomical_structure
Stereospecificity
chemistry
Drug Discovery
medicine
Benzoquinones
Molecular Medicine
Animals
Subjects
Details
- ISSN :
- 00222623
- Volume :
- 28
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....37dc495ec676d2090f880c2058a3bf09