Document Detail


The binding of SCH 39166 and SCH 23390 to 5-HT1C receptors in porcine choroid plexus.
MedLine Citation:
PMID:  1943454     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
SCH 39166 is a novel benzonaphthazepine, which has been characterized as a potent and selective D1 antagonist. Recently, its D1 selective benzazepine predecessor, SCH 23390, has been shown to bind to 5-HT1C binding sites in the choroid plexus. Therefore, the present studies were undertaken to determine if SCH 39166 has any measurable affinity for 5-HT1C binding sites. Our results indicate that SCH 39166 exhibited poor affinity for the 5-HT1C receptor, with a Ki of 1327 nM. In contrast, SCH 23390 inhibited [3H]-mesulergine binding to 5-HT1C receptors with a Ki of 30 nM. The non-selective 5-HT antagonist, methysergide, inhibited binding with a Ki of 2.4 nM. Finally, studies with the stereoisomers of SCH 39166 and SCH 23390 demonstrated that stereoselectivity at the 5-HT1C site is significantly less than for the D1 site.
Authors:
L A Taylor; C E Tedford; R D McQuade
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Life sciences     Volume:  49     ISSN:  0024-3205     ISO Abbreviation:  Life Sci.     Publication Date:  1991  
Date Detail:
Created Date:  1991-12-13     Completed Date:  1991-12-13     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  0375521     Medline TA:  Life Sci     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1505-11     Citation Subset:  IM    
Affiliation:
CV/CNS Pharmacology, Schering-Plough Research, Bloomfield NJ 07003.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antiparkinson Agents / metabolism
Benzazepines / metabolism*
Binding, Competitive
Choroid Plexus / metabolism*
Dopamine / metabolism
Dopamine Antagonists*
Ergolines / metabolism
Receptors, Serotonin / metabolism*
Serotonin Antagonists / metabolism
Swine
Chemical
Reg. No./Substance:
0/Antiparkinson Agents; 0/Benzazepines; 0/Dopamine Antagonists; 0/Ergolines; 0/Receptors, Serotonin; 0/Serotonin Antagonists; 112108-01-7/Sch 39166; 64795-35-3/CQ 32085

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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