ISSN:
1420-9071
Keywords:
5-hydroxytryptamine
;
serotonin
;
receptors
;
enteric nervous system
;
gut
;
radioautography
Source:
Springer Online Journal Archives 1860-2000
Topics:
Biology
,
Medicine
Notes:
Summary An enteric neural receptor for serotonin (5-HT) has been characterized. This receptor was assayed, using3H-5-HT as a radiologand, by rapid filtration of isolated enteric membranes and by radioautography. In addition, intracellular recordings were made from ganglion cells of the myenteric plexus. High affinity, saturable, reversible, and specific binding of3H-5-HT was demonstrated both to membranes of the dissected longitudinal muscle with adherent myenteric plexus and the mucosa-submucosa. Radioautographs showed these3H-5-HT binding sites to be in myenteric ganglia and in a broad unresolved band at the mucosal-submucosal interface. Antagonists active at receptors for other neurotransmitters than 5-HT, at either of the two known types of CNS 5-HT receptor, and at 5-HT uptake sites on serotonergic neurons failed to inhibit binding of3H-5-HT. The structural requirements of analogues for binding to the enteric 5-HT receptor matched the known pharmacology of M or neural 5-HT receptors. A novel 5-HT antagonist was found. This compound, N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan amide (5-HTP-DP), antagonized the action of 5-HT on type II/AH cells of the myenteric plexus but did not affect the release or actions of acetylcholine (nicotinic or muscarinic) or substance P. 5-HTP-DP was also an equally potent displacer of3H-5-HT from its binding sites on enteric membranes. It is concluded that the sites responsible for specific binding of3H-5-HT are enteric M or neural 5-HT receptors. These receptors differ from those now known to be present in the CNS.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01970002
