Document Detail

Agonist action of indole derivatives at 5-HT1-like, 5-HT3, and 5HT4 receptors in vitro.
MedLine Citation:
PMID:  1429745     Owner:  NLM     Status:  MEDLINE    
1. The potency of indole analogues has been studied, in vitro, at 5-hydroxytryptamine4 (5-HT4) receptors mediating contractions of guinea-pig ileum and relaxation of rat oesophagus. These have been compared to other 5-HT receptors in canine saphenous vein (5-HT1-like), rabbit aorta (5-HT2), and guinea-pig ileum (5-HT3). 2. At receptors mediating 5-HT4 responses in ileum and oesophagus, the rank orders of potency were similar. These rank orders differed from those observed at 5-HT1-like, 5-HT2, and 5-HT3 receptors. In particular, 5-hydroxy N,N, dimethyltryptamine but not 5-methoxy N,N, dimethyltryptamine acted as agonists at 5-HT4 receptors. At 5-HT1-like, 5-HT2 and 5-HT3 receptors these compounds were both active. 3. The 5-HT receptors mediating contractions of canine cephalic vein exhibited a rank order profile similar to that observed at receptors mediating contractions of canine saphenous vein, suggesting stimulation of a 5-HT1-like receptor. 4. The rank order of potency of the substituted indoles differed at 5-HT receptors mediating responses in canine saphenous vein, rabbit aorta and guinea-pig ileum (determined in the presence of 5-methoxytryptamine to desensitize 5-HT4 receptors), suggesting the presence of three distinct receptors. Indeed, at 5-HT3 receptors in the ileum, only three agonists (5-HT, 2-methyl-5-HT and 5-hydroxy N,N, dimethyltryptamine) elicited a response, while all remaining compounds were inactive. 5. It is concluded that rank orders of indole potency can prove useful in the delineation of 5-HT subtypes and together with differential antagonist affinities support the existence of four 5-HT receptor subtypes.
R M Eglen; L A Perkins; L K Walsh; R L Whiting
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Journal of autonomic pharmacology     Volume:  12     ISSN:  0144-1795     ISO Abbreviation:  J Auton Pharmacol     Publication Date:  1992 Oct 
Date Detail:
Created Date:  1992-12-04     Completed Date:  1992-12-04     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8106455     Medline TA:  J Auton Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  321-33     Citation Subset:  IM    
Institute of Pharmacology, Syntex Research, Palo Alto, California 94304.
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MeSH Terms
Aorta, Thoracic / drug effects
Cerebral Veins / drug effects
Esophagus / drug effects
Guinea Pigs
Ileum / drug effects
Indoles / pharmacology*
Muscle, Smooth / drug effects
Muscle, Smooth, Vascular / drug effects
Receptors, Serotonin / drug effects*
Saphenous Vein / drug effects
Serotonin Agonists / pharmacology*
Reg. No./Substance:
0/Indoles; 0/Receptors, Serotonin; 0/Serotonin Agonists

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