6-Substituted tricyclic partial ergoline compounds are selective and potent 5-hydroxytryptamine1A receptor agents
- 1. Stanford Univ. School of Medicine, CA (USA)
Description
A series of 6 tricyclic partial ergoline derivatives was analyzed using radioligand binding assays. Four agents (LY 178210, LY 254089, LY 197205, and LY 197206) display high affinity for 5-hydroxytryptamine1A (5-HT1A) receptor binding sites labeled by [3H]8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) and display ≥ 150 fold selectivity for the 5-HT1A over the 5-HT1D receptor binding site. The most potent agent investigated, LY 178210, is essentially inactive at a total of 12 other neurotransmitter receptor binding sites in the brain. Using a forskolin-stimulated adenylate cyclase assay as a model of 5-HT1A receptor function, LY 178210 was found to display partial agonist activity which was blocked by 10-5 M (-)pindolol. These data indicate that LY 178210 is a potent and selective 5-HT1A receptor partial agonist
Additional details
Publishing Information
- Journal Title
- Life Sciences
- Journal Volume
- 47
- Journal Issue
- 15
- Series
- Life Sci.
- Journal Page Range
- 1331-1337
- ISSN
- 0024-3205
- CODEN
- LIFSA
INIS
- Country of Publication
- United States
- Country of Input or Organization
- United States
- INIS RN
- 22028694
- Subject category
- S60: APPLIED LIFE SCIENCES;
- Descriptors DEI
- AFFINITY; BIOCHEMICAL REACTION KINETICS; BRAIN; RADIOASSAY; RECEPTORS; SEROTONIN; SYMPATHOLYTICS; TRACER TECHNIQUES; TRITIUM COMPOUNDS
- Descriptors DEC
- AMINES; AUTONOMIC NERVOUS SYSTEM AGENT; AZOLES; BODY; CENTRAL NERVOUS SYSTEM; DRUGS; HETEROCYCLIC COMPOUNDS; HYDROGEN COMPOUNDS; HYDROXY COMPOUNDS; INDOLES; ISOTOPE APPLICATIONS; KINETICS; NERVOUS SYSTEM; NEUROREGULATORS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANS; PYRROLES; RADIOPROTECTIVE SUBSTANCES; REACTION KINETICS; RESPONSE MODIFYING FACTORS; SYMPATHOMIMETICS; TRYPTAMINES