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Title: Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20

Abstract

Pharmacological characterization of the serotonin activation of adenylate cyclase in membrane preparation using over 40 serotonergic and non-serotonergic compounds demonstrated that the receptor mediating the response was distinct from previously described mammalian serotonin receptors. Agonist activity was only observed with tryptamine and ergoline derivatives. Potent antagonism was observed with several ergoline derivatives and with compounds such as mianserin and methiothepine. A comparison of the rank order of potency of a variety of compounds for the NCB.20 cell receptor with well characterized mammalian and non-mammalian serotonin receptors showed a pharmacological similarity, but not identity, with the mammalian 5-HT{sub 1C} receptor, which modulates phosphatidylinositol metabolism, and with serotonin receptors in the parasitic trematodes Fasciola hepatica and Schistosoma mansoni, which are coupled to adenylate cyclase. Equilibrium binding analysis utilizing ({sup 3}H)serotonin, ({sup 3}H)lysergic acid diethylamide or ({sup 3}H)dihydroergotamine demonstrated that there are no abundant high affinity serotonergic sites, which implies that the serotonin activation of adenylate cyclase is mediated by receptors present in low abundance. Incubation of intact NCB.20 cells with serotinin resulted in a time and concentration dependent desensitization of the serotonin receptor.

Authors:
Publication Date:
Research Org.:
Stanford Univ., CA (USA)
OSTI Identifier:
7003290
Resource Type:
Thesis/Dissertation
Resource Relation:
Other Information: Thesis (Ph. D.)
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; CYCLASES; ENZYME ACTIVITY; RECEPTORS; CHEMICAL COMPOSITION; SEROTONIN; BIOCHEMICAL REACTION KINETICS; CELL MEMBRANES; DOSE-RESPONSE RELATIONSHIPS; LYSERGIC ACID; TIME DEPENDENCE; TRACER TECHNIQUES; TREMATODES; TRITIUM COMPOUNDS; TUMOR CELLS; ALKALOIDS; AMINES; ANIMAL CELLS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; AZAARENES; AZOLES; CARBOXYLIC ACIDS; CELL CONSTITUENTS; DRUGS; ENZYMES; HELMINTHS; HETEROCYCLIC ACIDS; HETEROCYCLIC COMPOUNDS; HYDROGEN COMPOUNDS; HYDROXY COMPOUNDS; INDOLES; ISOTOPE APPLICATIONS; KINETICS; LYASES; MEMBRANE PROTEINS; MEMBRANES; NEUROREGULATORS; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; PLATYHELMINTHS; PROTEINS; PYRROLES; RADIOPROTECTIVE SUBSTANCES; REACTION KINETICS; SYMPATHOMIMETICS; TRYPTAMINES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Conner, D.A. Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20. United States: N. p., 1988. Web.
Conner, D.A. Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20. United States.
Conner, D.A. Fri . "Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20". United States.
@article{osti_7003290,
title = {Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20},
author = {Conner, D.A.},
abstractNote = {Pharmacological characterization of the serotonin activation of adenylate cyclase in membrane preparation using over 40 serotonergic and non-serotonergic compounds demonstrated that the receptor mediating the response was distinct from previously described mammalian serotonin receptors. Agonist activity was only observed with tryptamine and ergoline derivatives. Potent antagonism was observed with several ergoline derivatives and with compounds such as mianserin and methiothepine. A comparison of the rank order of potency of a variety of compounds for the NCB.20 cell receptor with well characterized mammalian and non-mammalian serotonin receptors showed a pharmacological similarity, but not identity, with the mammalian 5-HT{sub 1C} receptor, which modulates phosphatidylinositol metabolism, and with serotonin receptors in the parasitic trematodes Fasciola hepatica and Schistosoma mansoni, which are coupled to adenylate cyclase. Equilibrium binding analysis utilizing ({sup 3}H)serotonin, ({sup 3}H)lysergic acid diethylamide or ({sup 3}H)dihydroergotamine demonstrated that there are no abundant high affinity serotonergic sites, which implies that the serotonin activation of adenylate cyclase is mediated by receptors present in low abundance. Incubation of intact NCB.20 cells with serotinin resulted in a time and concentration dependent desensitization of the serotonin receptor.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1988},
month = {1}
}

Thesis/Dissertation:
Other availability
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